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  2. Epigenetics Autophagy PROTAC
  3. Epigenetic Reader Domain Autophagy Ligands for Target Protein for PROTAC
  4. (+)-JQ-1

(+)-JQ-1  (Synonyms: JQ1)

目錄號(hào): HY-13030 純度: 99.90%
COA 產(chǎn)品使用指南

(+)-JQ-1 (JQ1) 是一種有效特異性的可逆 BET bromodomain 抑制劑，抑制 BRD4(1/2) 的 IC50 分別為 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。

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(+)-JQ-1 Chemical Structure

(+)-JQ-1 Chemical Structure

CAS No. : 1268524-70-4

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥935
In-stock
5 mg ￥850
In-stock
10 mg ￥1100
In-stock
50 mg ￥2250
In-stock
100 mg ￥3600
In-stock
200 mg ￥4350
In-stock
500 mg ￥5920
In-stock
1 g   詢(xún)價(jià)  
5 g   詢(xún)價(jià)  

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Customer Review

Other Forms of (+)-JQ-1:

MCE 顧客使用本產(chǎn)品發(fā)表的 232 篇科研文獻(xiàn)

WB
IHC

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2022 Nov 11;41(1):321.  [Abstract]

    The expression of BRD4 and MYC proteins are each downregulated by JQ1 (0.5 μM; 24 h) or panobinostat (PAN; 10 nM; 24 h) alone, and more profoundly by the combination of these two inhibitors in in MB HD-MB03 and D-283 cells.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Res. 2019 Jan 1;79(1):251-262.  [Abstract]

    Cleavage of PARP is assessed by western blotting with the treatment of JQ 1.

    (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430.  [Abstract]

    Immunoblots (IB) are done to detect γH2AX and DNA repair proteins, Ku80 and RAD51 using UAB-PA4 or UAB-PA16 tumors harvested from mice 24 h following final treatment. Quantitation by densitometry of results is shown below each IB image.

    (+)-JQ-1 purchased from MCE. Usage Cited in: EBioMedicine. 2019 Jun;44:419-430.  [Abstract]

    Panc1 or MiaPaCa2 cells are exposed to JQ1 (0.5, 1, 5, or 10 μM) for 48 h, and immunoblotted for γH2AX.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan;134:96-106.  [Abstract]

    Western blot analysis of p21 and G2/M regulatory molecules, cyclin B1, CDC2, p-CDC2 (Tyr-15) and CDC25A in the treatment of NL101 and BMN673.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Eur J Pharm Biopharm. 2019 Jan;134:96-106.  [Abstract]

    Western blot of cleaved Caspase-3 and cleaved PARP-1 in AML cells with the treatment of NL101 and BMN673.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cell. 2018 Sep 20;175(1):186-199.e19.  [Abstract]

    Cells are treated with EPZ-6438 (1 μM) or GSK126 (1 μM) for 6 days. Protein levels are analyzed by immunoblotting. Cells are treated with EPZ-6438 (1 μM), JQ1 (0.25 μM) alone or combination for 6 days. Protein levels are analyzed by immunoblotting.

    (+)-JQ-1 purchased from MCE. Usage Cited in: EMBO Mol Med. 2018 Apr;10(4). pii: e8163.  [Abstract]

    Western blot analysis of MYC and FGFR3 expression in lysates from MGH-U3 and RT112 cells treated with (+)-JQ1 (1 or 4 μM) for 48 h. Anti-actin antibody is used as a loading control. Pan-FGFR inhibitor, PD173074 (50 nM and 1 μM), and inactive enantiomer (-)-JQ1 (4 μM) are used as controls.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:195-207.  [Abstract]

    Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 10;419:64-74.  [Abstract]

    ESCC cell lines are treated with 500 nM JQ1 for 48 h, whole cell lysates are analyzed by western blotting. The expressions of p21 and p27 are further upregulated by JQ1 concomitant with cell cycle arrest at G1 phase.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2018 Oct 28;435:44-54.  [Abstract]

    H157, H1299, and HCT116 cells are harvested for preparation of whole-cell protein lysates and subsequent Western blotting to detect the indicated proteins.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.  [Abstract]

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625.  [Abstract]

    ARID1A Western blot analysis of ARID1A protein levels in the ES2 polyclonal ARID1A knockout clone and ES2/OVCA429 monoclonal ARID1A knockout clones.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncogene. 2018 Aug;37(33):4611-4625.  [Abstract]

    The OVCA429 cells are subjected to Western blot analysis for the indicated proteins. ACTIN servea as a loading control.

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Med Chem. 2018 Jan 25;61(2):504-513.  [Abstract]

    Protein degradation profile of VHL-based BET degraders. Sub-confluent HeLa cells are treated for 24 h with varying concentration of test compounds JQ1(Compound 3), I-BET726 (Compound 4). Protein extracts are separated by SDS-PAGE and then analyzed by Western blot. Proteins Brd4, Brd3, Brd2 and β-actin are probed for JQ1and I-BET726 with specific antibodies.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.  [Abstract]

    Western blot detection of the p-TEFb component CDK9, Cyclin T1 and CDK9 phosphorylation on Thr186, as well as its downstream RNA poly II CTD and phosphate CTD after J-Lat 10.6 cells are treated with PR-957 in dose-dependent manner.

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2018 Dec 7;127:83-96.  [Abstract]

    The expression of EndMT-related proteins, VE-cadherin, CD31, vimentin, α-SMA and FSP1, were compared among Ctrl, JQ1(-), JQ1, TGF-β1, and TGF-β1+JQ1 groups in both HUVECs and MAECs.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Sci Rep. 2018 Aug 1;8(1):11554.  [Abstract]

    A549 cells are mock-treated (0.1% DMSO in culture medium) or treated with RVX-208 at 500?nM, PFI-1 at 500?nM, JQ1 at 300?nM, or with 300?nM (-)-JQ1, an inactive enantiomer of JQ1. The cells are then infected with Ad2 at 1 PFU/cell for 24?h. Viral hexon and penton base (PB) protein is detected by immunoblotting analysis.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Biol Ther. 2018 May 4;19(5):407-415.  [Abstract]

    NSCLC cells are treated with 0-8 μM JQ1 for 24h, then the whole-cell lysates are prepared and subjected to western blot assay.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Oncotarget. 2018 May 1;9(33):23003-23017.  [Abstract]

    The expression of MYC protein is markedly repressed in JQ1-treated ccRCC cells (2.5 and 5 μM) in comparison with that in mock cells. β-Actin is used as a loading control. Densitometry analyses using ImageJ software are performed.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Leukemia. 2017 Oct;31(10):2037-2047.  [Abstract]

    Immunoprecipitation with anti-BIM antibody illustrates the increased binding of BIM to BCL-2 after JQ1 treatment.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Aug 28;402:100-109.  [Abstract]

    Expression and activation statuses of signal proteins in three BRAFV600E-mutant colon cancer cell lines treated with either RG7204, JQ1, or their combination. Phosphorylation of CRAF and AKT is suppressed by JQ1 in RKO cells and possibly in Colo205 cells (green arrow heads).

    (+)-JQ-1 purchased from MCE. Usage Cited in: Genome Res. 2017 Nov;27(11):1830-1842.  [Abstract]

    Ki67 immunohistochemistry and H&E stained sections from representative xenograft per treatment arm. A marked decrease in the proliferation marker Ki67 is observed in xenografts treated with JQ1.

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Cell Biochem. 2017 Aug;118(8):2182-2192.  [Abstract]

    JQ1 induces G0/G1 cell cycle arrest and apoptosis of chondrosarcoma cells via regulating p21, p27, Cyclin E2, and Cyclin D1 expression. (A and B) JQ1 regulates the expression of cell cycle regulators such as p21, p27, Cyclin E2, and Cyclin D1. SW 1353 and Hs 819.T cells are seeded into a 6-well plate for 72 h, then the cells are treated with different concentrations of JQ1 (JQ1#1: 200 nM; JQ1#2: 2 μM; JQ1#3: 20 μM) for another 24 h. Total cell lysate is used for the analysis of protein expressio

    (+)-JQ-1 purchased from MCE. Usage Cited in: Metabolism. 2016 Oct;65(10):1478-88.  [Abstract]

    The BRD4 protein level in the liver is significantly suppressed by force-feeding fructose or glucose with (+)-JQ1. Protein levels of Brd4 in the liver of mice force-fed with glucose or fructose, with or without (+)-JQ1. Quantification of protein levels is performed by normalization against the level of β-actin (n = 6).

    (+)-JQ-1 purchased from MCE. Usage Cited in: PLoS Pathog. 2016 Oct 20;12(10):e1005950.  [Abstract]

    Dose effect of JQ1 on HSV infection. Vero cells are treated with JQ1 at concentrations as indicated. HSV-1 or HSV-2 at 1 MOI are used. The samples are used for protein expression analysis by western blot.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Jun;15(6):1217-26.  [Abstract]

    JQ1-mediated c-MYC repression correlates with growth inhibition. BETi preferentially inhibit c-MYC protein expression in sensitive cell lines. JQ1-sensitive GP5D, HT29 and LIM1215 cells and JQ1-resistant KM12, SW480 and HuTu80 cells where treated with JQ1 (500 nM) for 2-24 hours and c-MYC protein expression determined by western blot.

    (+)-JQ-1 purchased from MCE. Usage Cited in: J Biol Chem. 2016 Nov 4;291(45):23756-23768.  [Abstract]

    BET inhibition blocks growth of TNBC cells without consistently downregulating MYC. Western blot analysis of MYC expression levels in TNBC cell lines treated for 24 hours with vehicle or 500 nM JQ1. Values on the western blot are relative to the vehicle-treated 1143 sample following normalization to β-actin.

    (+)-JQ-1 purchased from MCE. Usage Cited in: Biochim Biophys Acta. 2016 Dec;1859(12):1527-1537.  [Abstract]

    JQ1 treatment decreases β-catenin levels in HCT116 cells, but increases TAZ protein. When cells reach confluence, they are serum-starved overnight and pretreated with DMSO or JQ1 (500 nM) for 1 hour, followed by growth medium (containing 10% serum) stimulation for 24 hours.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2))[1]. (+)-JQ-1 also activates autophagy[2].

    IC50 & Target

    IC50: 77/33 nM (BRD4(1/2))[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    697 EC50
    0.09 μM
    Compound: 1; (+)-JQ1
    Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    A-375 IC50
    7.5 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    A549 IC50
    1.67 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human A549 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    A549 IC50
    13.1 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    A549 EC50
    17 μM
    Compound: (+)-JQ1
    Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay
    Cytotoxicity against human A549 cells assessed as viable cells incubated for 23 hrs by alamar blue assay
    		[PMID: 35007061]
    ASPC1 IC50
    3.39 μM
    Compound: JQ1
    Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay
    Antiproliferative activity against human ASPC1 cells assessed as cell growth inhibition incubated for 6 days by MTS assay
    		[PMID: 35500243]
    CAPAN-1 IC50
    0.45 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    CAPAN-1 IC50
    0.58 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    		[PMID: 35091172]
    CAPAN-1 IC50
    2.44 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    		[PMID: 35091172]
    CAPAN-1 IC50
    2.44 μM
    Compound: JQ-1
    Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay
    Antiproliferative activity against human CAPAN-1 cells assessed as reduction in cell viability after 4 days by MTT assay
    		[PMID: 34813314]
    CAPAN-1 IC50
    24.1 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay
    Antiproliferative activity against human CAPAN-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay
    		[PMID: 35091172]
    CFPAC-1 IC50
    0.35 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    CFPAC-1 IC50
    1.56 μM
    Compound: JQ-1
    Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay
    Antiproliferative activity against human CFPAC-1 cells assessed as reduction in cell viability after 4 days by MTT assay
    		[PMID: 34813314]
    CFPAC-1 IC50
    1.56 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    		[PMID: 35091172]
    CFPAC-1 IC50
    1.86 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    		[PMID: 35091172]
    CFPAC-1 IC50
    13.9 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay
    Antiproliferative activity against human CFPAC-1 cells assessed as inhibition of cell growth measured after 3 days by MTT assay
    		[PMID: 35091172]
    CT26 IC50
    28.67 μM
    Compound: 1; JQ1
    Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Antiproliferative activity against human CT26 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    		[PMID: 33862375]
    CWR22R IC50
    0.033 μM
    Compound: 1, JQ1
    Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay
    Antiproliferative activity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay
    		[PMID: 34999525]
    CWR22R IC50
    0.071 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    CWR22R IC50
    0.071 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    		[PMID: 29541371]
    DU-145 IC50
    2.52 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human DU145 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    DU-145 IC50
    2.52 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    Antiproliferative activity against human DU145 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    		[PMID: 29541371]
    HCT-116 IC50
    2.03 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against BRCA2-mutated human HCT-116 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    HCT-116 IC50
    4.212 μM
    Compound: 1; JQ1
    Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Antiproliferation activity against human HCT116 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 33214826]
    HEK-293T IC50
    107 nM
    Compound: JQ1
    Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
    Inhibition of cell growth in HEK293T cells incubated for 72 hrs by CellTiter-blue reagent based assay
    		[PMID: 34710325]
    HeLa IC50
    > 100 μM
    Compound: 1, (+)-JQ1
    Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay
    Cytotoxicity against human HeLa cells after 24 hrs by WST-1 assay
    		[PMID: 23517011]
    HeLa IC50
    3.76 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human HeLa cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    HepG2 IC50
    11.3 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    HepG2 IC50
    18.39 μM
    Compound: 1; JQ1
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    		[PMID: 33862375]
    HFL1 IC50
    0.29 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against HFL1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    HL-60 GI50
    0.021 μM
    Compound: 15; (+)-JQ1
    Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    		[PMID: 33275431]
    HL-60 IC50
    0.06 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human HL60 cells after 72 hrs by CCK8 assay
    		[PMID: 26731490]
    HL-60 IC50
    0.11 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against BRD4-sensitive human HL60 cells after 72 hrs by CCK8 assay
    		[PMID: 28314513]
    HL-60 IC50
    0.16 μM
    Compound: 1; (+)-jQ1
    Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay
    		[PMID: 32883643]
    HL-60 EC50
    0.2 μM
    Compound: (+)-JQ1
    Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis
    Induction of ATRA-induced human HL60 cell differentiation pretreated for 1 hr followed by ATRA addition measured after 3 days by Wright-Giemsa staining based microscopic analysis
    		[PMID: 28549889]
    HL-60 IC50
    0.87 μM
    Compound: 2; JQ1
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability by MTT assay
    		[PMID: 31857846]
    HL-60 IC50
    2.91 μM
    Compound: (+)-JQ-1
    Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK-8 assay
    		[PMID: 31079968]
    HL-60 IC50
    3.46 μM
    Compound: (+)-JQ-1
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 32631570]
    HL-60 IC50
    5.3 μM
    Compound: 3; (+)-JQ1
    Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    Hs-578T IC50
    0.16 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human Hs578T cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    HT-29 IC50
    0.02 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human HT-29 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    HT-29 IC50
    0.104 μM
    Compound: 1, (+)-JQ1
    Growth inhibition of human HT-29 cells after 72 hrs by SRB assay
    Growth inhibition of human HT-29 cells after 72 hrs by SRB assay
    		[PMID: 25559428]
    HT-29 IC50
    0.28 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by CCK8 assay
    		[PMID: 26731490]
    HT-29 IC50
    0.48 μM
    Compound: 1; (+)-jQ1
    Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay
    		[PMID: 32883643]
    HT-29 IC50
    19.6 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    K562 IC50
    > 2000 nM
    Compound: 1, JQ-1
    Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    		[PMID: 26080064]
    K562 IC50
    0.64 μM
    Compound: 2; (+-)JQ1
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay
    		[PMID: 27142751]
    K562 IC50
    9.12 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against BRD4-independent human K562 cells after 72 hrs by CCK8 assay
    		[PMID: 28314513]
    L02 IC50
    54.2 μM
    Compound: (+)-JQ1
    Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell growth measured after 24 hrs by MTT assay
    		[PMID: 30926312]
    LNCaP IC50
    0.16 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    LNCaP IC50
    0.16 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    		[PMID: 29541371]
    LNCaP C4-2B IC50
    0.19 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    LNCaP C4-2B IC50
    0.19 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    		[PMID: 29541371]
    LOUCY EC50
    0.09 μM
    Compound: 1; (+)-JQ1
    Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human Loucy cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    MCF7 GI50
    > 50 μM
    Compound: 15; (+)-JQ1
    Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    		[PMID: 33275431]
    MCF7 IC50
    0.2 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human MCF7 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    MCF7 IC50
    38 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    MCF7:CFR IC50
    90 nM
    Compound: 1; JQ1
    Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis
    Growth inhibition of fulvestrant-resistant human MCF7:CFR cells measured after 5 days by Hoechst 33342 dye based imaging analysis
    		[PMID: 32453591]
    MDA-MB-231 IC50
    0.64 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against BRCA-proficient human MDA-MB-231 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    MDA-MB-231 IC50
    0.64 μM
    Compound: JQ-1
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days
    Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability after 7 days
    		[PMID: 34813314]
    MDA-MB-231 IC50
    29.51 μM
    Compound: 1; JQ1
    Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
    		[PMID: 34908415]
    MDA-MB-468 IC50
    0.54 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against BRCA-proficient human MDA-MB-468 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    MDA-MB-468 IC50
    30.19 μM
    Compound: 1; JQ1
    Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
    		[PMID: 34908415]
    MM1.S IC50
    0.019 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay
    		[PMID: 28586718]
    MM1.S IC50
    0.02 μM
    Compound: 2; (+)-JQ1
    Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MM1S cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 28535045]
    MM1.S IC50
    0.062 μM
    Compound: JQ1
    Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
    Antiproliferative activity against human MM1.S cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
    		[PMID: 36563515]
    MM1.S IC50
    0.109 μM
    Compound: 1, (+)-JQ1
    Growth inhibition of human MM1S cells after 72 hrs by SRB assay
    Growth inhibition of human MM1S cells after 72 hrs by SRB assay
    		[PMID: 25559428]
    MM1.S IC50
    29.8 nM
    Compound: (+)-JQ-1; 1
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay
    		[PMID: 31490070]
    MM1.S IC50
    33 nM
    Compound: JQ1
    Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
    Inhibition of cell growth in human MM1.S cells incubated for 72 hrs by CellTiter-blue reagent based assay
    		[PMID: 34710325]
    MM1.S IC50
    69.1 nM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay
    		[PMID: 29525435]
    MOLM-13 IC50
    56 nM
    Compound: 1, JQ-1
    Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    		[PMID: 26080064]
    MOLM-13 IC50
    56 nM
    Compound: 1; JQ-1
    Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
    Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay
    		[PMID: 28463487]
    MV4-11 IC50
    0.012 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 assay
    		[PMID: 26731490]
    MV4-11 IC50
    0.017 μM
    Compound: 1, JQ1
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 96 to 120 hrs by celltiter glo assay
    		[PMID: 34999525]
    MV4-11 IC50
    0.023 μM
    Compound: 1, (+)-JQ1
    Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay
    Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay
    		[PMID: 25559428]
    MV4-11 IC50
    0.042 μM
    Compound: JQ1
    Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
    Antiproliferative activity against human MM4-11 cells assessed as inhibition of cell growth incubated for 72 hrs MTS assay
    		[PMID: 36563515]
    MV4-11 IC50
    0.06 μM
    Compound: Cpd X1; (+)-JQ1
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay
    		[PMID: 31421967]
    MV4-11 IC50
    0.08 μM
    Compound: (+)-JQ1
    Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against BRD4-sensitive human MV411 cells after 72 hrs by CCK8 assay
    		[PMID: 28314513]
    MV4-11 GI50
    0.08 μM
    Compound: (+)-JQ-1
    Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay
    Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay
    		[PMID: 26191363]
    MV4-11 IC50
    0.08082 μM
    Compound: 1; JQ1
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 48 hrs by CellTiter-Glo assay
    		[PMID: 31767403]
    MV4-11 IC50
    0.157 μM
    Compound: (+)-JQ-1
    Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 72 hrs by CellTiter-Glo assay
    		[PMID: 34731760]
    MV4-11 IC50
    0.16 μM
    Compound: (+)-JQ-1
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    		[PMID: 32631570]
    MV4-11 IC50
    0.16 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human MV4-11 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    MV4-11 IC50
    0.24 μM
    Compound: 2; (+-)JQ1
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by Alamar blue assay
    		[PMID: 27142751]
    MV4-11 IC50
    0.242 μM
    Compound: 1, (+)-JQ1
    Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay
    Cytotoxicity against human MV4-11 cells after 72 hrs by MTS assay
    		[PMID: 23517011]
    MV4-11 IC50
    0.57 μM
    Compound: (+)-JQ-1
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CCK-8 assay
    		[PMID: 31079968]
    MV4-11 IC50
    24 nM
    Compound: 1, JQ-1
    Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay
    		[PMID: 26080064]
    MV4-11 IC50
    24 nM
    Compound: 1; JQ-1
    Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay
    Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay
    		[PMID: 28463487]
    MV4-11 IC50
    6.4 μM
    Compound: 3; (+)-JQ1
    Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    MX1 EC50
    0.144 μM
    Compound: 1; (+)-JQ1
    Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay
    Inhibition of BRD4 in human MX1 cells assessed as decrease in cell proliferation after 3 days by Celltiter-Glo assay
    		[PMID: 31303996]
    MX1 EC50
    254 nM
    Compound: 1b; JQ1
    Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
    Antiproliferative activity against human MX1 cells after 72 hrs by Cell Titer Glo assay
    		[PMID: 28949521]
    NALM-6 EC50
    0.06 μM
    Compound: 1; (+)-JQ1
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay
    		[PMID: 29170024]
    NCI-H1975 IC50
    1.23 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human NCI-H1975 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    NRK-49F IC50
    21.1 μM
    Compound: (+)-JQ1
    Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    Antifibrotic activity against rat NRK-49F cells assessed as reduction in cell growth measured after 48 hrs by MTT assay
    		[PMID: 30926312]
    PC-3 IC50
    3.01 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human PC3 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    PC-3 IC50
    3.01 μM
    Compound: 1; (+)-JQ1
    Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    Antiproliferative activity against human PC3 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay
    		[PMID: 29541371]
    Raji IC50
    0.069 μM
    Compound: 2, (+)-JQ1
    Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs
    Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs
    		[PMID: 24900758]
    SK-MEL-5 GI50
    > 40 μM
    Compound: 15; (+)-JQ1
    Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
    		[PMID: 33275431]
    SW1990 IC50
    0.63 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 7 days by MTT assay
    		[PMID: 35091172]
    SW1990 IC50
    1.11 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 5 days by MTT assay
    		[PMID: 35091172]
    SW1990 IC50
    3.74 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth measured after 4 days by MTT assay
    		[PMID: 35091172]
    SW1990 IC50
    3.74 μM
    Compound: JQ-1
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay
    Antiproliferative activity against human SW1990 cells assessed as reduction in cell viability after 4 days by MTT assay
    		[PMID: 34813314]
    SW1990 IC50
    31.6 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay
    Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth after 3 days by MTT assay
    		[PMID: 35091172]
    T-cell IC50
    0.11 μM
    Compound: 6m; JQ1
    Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay
    Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay
    		[PMID: 26869194]
    THP-1 IC50
    0.33 μM
    Compound: (+)-JQ1
    Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay
    Antiproliferative activity against human THP-1 cells expressing BRD4 assessed as inhibition of cell growth measured after 3 days by MTT assay
    		[PMID: 35091172]
    THP-1 IC50
    0.56 μM
    Compound: JQ-1
    Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA
    Antiinflammatory activity against human THP-1 cells assessed as inhibition of LPS-induced IL-6 production incubated for 18 hrs by ELISA
    		[PMID: 35318165]
    U-266 IC50
    3.45 μM
    Compound: 1; JQ1
    Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Antiproliferative activity against human U-266 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    		[PMID: 33862375]
    U2OS IC50
    > 100 μM
    Compound: 1, (+)-JQ1
    Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay
    Cytotoxicity against human U2OS cells after 24 hrs by WST-1 assay
    		[PMID: 23517011]
    U2OS IC50
    1.62 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human U2OS cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    U-937 IC50
    > 20 μM
    Compound: 3; (+)-JQ1
    Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    Cytotoxicity against human U937 cells assessed as decrease in cell viability after 24 hrs by MTT assay
    		[PMID: 27266999]
    VCaP IC50
    0.012 μM
    Compound: 1; (+)-JQ-1
    Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay
    		[PMID: 29758518]
    WI-38 IC50
    4.97 μM
    Compound: 1; (+)-jQ1
    Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay
    		[PMID: 32883643]
    體外研究
    (In Vitro)

    (+)-JQ-1 代表溴結(jié)構(gòu)域 BET 家族的一種有效、高度特異性和 Kac 競(jìng)爭(zhēng)性抑制劑。(+)- JQ-1 (100 nM，48 h) 促進(jìn)鱗狀分化，表現(xiàn)為細(xì)胞紡錘形、扁平化和角蛋白表達(dá)增加。與 (-)-JQ1 (250 nM) 和載體對(duì)照相比，(+)-JQ-1 (250 nM) 在經(jīng)處理的 NMC 797 細(xì)胞中誘導(dǎo)角蛋白的快速表達(dá)，如通過(guò)定量免疫組織化學(xué)所確定的。(+)-JQ-1 (與 (-)-JQ1 (250 nM) 相比) 會(huì)引發(fā)經(jīng)處理的 NMC 797 細(xì)胞的時(shí)間依賴(lài)性強(qiáng) (3+) 角蛋白染色[1]。添加 (+)-JQ-1 后幾乎立即觀察到自噬基因的去抑制[2]。(+)-JQ-1 是 BET 家族共激活蛋白 BRD4 的一種有效的噻吩二氮卓抑制劑 (Kd=90 nM)，通過(guò) MYC 致癌基因的轉(zhuǎn)錄控制參與癌癥的發(fā)病機(jī)制。(+)-JQ-1 的劑量范圍研究證明有效抑制 H4Kac4 結(jié)合，小鼠 BRDT (1) 的 IC50 值為 10 nM，人 BRDT (1) 的 IC50 值為 11 nM[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    已確定腫瘤的匹配小鼠隊(duì)列隨機(jī)接受 (+)-JQ1 (50 mg/kg) 或載體處理，每日腹膜內(nèi)注射。在隨機(jī)化之前和處理四天之后，通過(guò) FDG-PET 成像評(píng)估小鼠。(+)-JQ1 處理觀察到 FDG 攝取顯著減少。腫瘤體積測(cè)量證實(shí) JQ1 處理可減少腫瘤生長(zhǎng)。(+)-JQ1 的藥代動(dòng)力學(xué)研究是在 CD1 小鼠靜脈內(nèi)和口服給藥后進(jìn)行的。靜脈內(nèi)給藥 (5 mg/kg) 后 (+)-JQ1 的平均血漿濃度-時(shí)間曲線。靜脈內(nèi) (+)-JQ1 的藥代動(dòng)力學(xué)參數(shù)顯示出出色的藥物暴露 (AUC=2090 hr*ng/mL) 和大約一小時(shí)的半衰期 (T1/2)。制定口服給藥 (10 mg/kg) 后 (+)-JQ1 的平均血漿濃度-時(shí)間曲線。口服 (+)-JQ1 的藥代動(dòng)力學(xué)參數(shù)表現(xiàn)出出色的口服生物利用度 (F=49%)、血漿峰濃度 (Cmax=1180 ng/mL) 和藥物暴露量 (AUC=2090 hr*ng)/mL)[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    456.99

    Formula

    C23H25ClN4O2S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : ≥ 45 mg/mL (98.47 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開(kāi)封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.1882 mL 10.9412 mL 21.8823 mL
    5 mM 0.4376 mL 2.1882 mL 4.3765 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.47 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.47 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 20% HP-β-CD in Saline

      Solubility: 10 mg/mL (21.88 mM); 懸濁液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (21.88 mM); 澄清溶液; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.90%

    參考文獻(xiàn)
    Cell Assay
    [1]

    NUT midline carcinoma patient cell lines (797 and 11060) are plated in T-25 flasks and grown in DMEM (797) or RPMI (11060) containing 10 % fetal bovine serum. Cells are treated with either 250 nM (+)-JQ1, 250 nM (-)-JQ1 or the equivalent volume of DMSO (0.025%). At the desired time point, 2×106 cells are spun at 500× g for 5 minutes at 4°C and washed with PBS. Pellets are resuspended in 1 mL of cold PBS and added dropwise while gently vortexing to 9 mL 70 % ethanol in a 15 mL polypropylene centrifuge tube. Fixed cells are then frozen at -20°C overnight. The next day, cells are centrifuged at 500× g for 10 minutes at 4°C and washed with 3 mL of cold PBS. Cells are resuspended in 500 μL of propidium iodide staining solution (0.2 mg/mL RNAse A, 0.02 mg/mL propidium iodide, 0.1 % Triton-X in PBS) and incubated for 20 minutes at 37°C. Samples are then transferred to ice and analyzed on a BD FACS Canto II. Histograms are generated and cell cycle analysis is performed using FlowJo flow cytometry analysis software[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Mice[1]
    Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Male CD1 mice (24-29 g) are treated with a single dose of (+)-JQ1 at 5 mg/kg for intravenous tail vein injection studies and 10 mg/kg for oral gavage studies.
    Rats[3]
    Adult male Sprague-Dawley rats are treated with vehicle or (+)-JQ1 (10 mg/kg). Treatment is administered IP at 1/100 body mass. Rats are checked twice-daily for mortality and weighed on days 1, 3, 7, 14, and 21. The treatment regimen utilized 4 days of 50 mg/kg JQ1 administered daily which is decreased to 10 mg/kg twice daily for the remainder of the study due to the appearance of adverse effects in a subset of animals. For all animals completing 3 weeks of treatment, testis mass, sperm motility, and sperm counts are determined as described for mouse studies. In brief, testes are fixed in Bouin’s and prepared for histology. The other half is minced in warm M16 buffer and used for sperm counts and motility studies.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 1 year; -20°C, 6 months。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1882 mL 10.9412 mL 21.8823 mL 54.7058 mL
    5 mM 0.4376 mL 2.1882 mL 4.3765 mL 10.9412 mL
    10 mM 0.2188 mL 1.0941 mL 2.1882 mL 5.4706 mL
    15 mM 0.1459 mL 0.7294 mL 1.4588 mL 3.6471 mL
    20 mM 0.1094 mL 0.5471 mL 1.0941 mL 2.7353 mL
    25 mM 0.0875 mL 0.4376 mL 0.8753 mL 2.1882 mL
    30 mM 0.0729 mL 0.3647 mL 0.7294 mL 1.8235 mL
    40 mM 0.0547 mL 0.2735 mL 0.5471 mL 1.3676 mL
    50 mM 0.0438 mL 0.2188 mL 0.4376 mL 1.0941 mL
    60 mM 0.0365 mL 0.1824 mL 0.3647 mL 0.9118 mL
    80 mM 0.0274 mL 0.1368 mL 0.2735 mL 0.6838 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    產(chǎn)品名稱(chēng)：
    (+)-JQ-1
    目錄號(hào)：
    HY-13030
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