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  2. Metabolic Enzyme/Protease Autophagy Apoptosis
  3. Proteasome Autophagy Apoptosis
  4. MG-132

MG-132  (Synonyms: Z-Leu-Leu-Leu-al; MG132)

目錄號(hào): HY-13259 純度: 99.97%
COA 產(chǎn)品使用指南

MG-132 (Z-Leu-Leu-Leu-al) 是一種有效的，可逆的蛋白酶體 (proteasome) 抑制劑，IC50 為 100 nM。MG-132 有效阻斷 26S 蛋白酶體復(fù)合物的蛋白水解活性。MG-132 是一種肽醛，是自噬 (autophagy) 激活劑。MG-132 還誘導(dǎo)凋亡 (apoptosis)。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

MG-132 Chemical Structure

MG-132 Chemical Structure

CAS No. : 133407-82-6

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Customer Review

Other Forms of MG-132:

MCE 顧客使用本產(chǎn)品發(fā)表的 1104 篇科研文獻(xiàn)

WB

    MG-132 purchased from MCE. Usage Cited in: Pharmacol Res. 2023 Feb 20;189:106704.  [Abstract]

    MG132 (10 μM) significantly reduces the degradation of YTHDC1 protein mediated by Dihydroartemisinin (DHA) in HSCs.

    MG-132 purchased from MCE. Usage Cited in: J Ethnopharmacol. 2023 Feb 13;307:116243.  [Abstract]

    Both MG-132 (10 μM) and Baf A1 (10 μM) markedly increase TGF-β1 protein expression in HG-stimulated SV40-MES-13 cells (Fig. C and D).

    MG-132 purchased from MCE. Usage Cited in: J Virol. 2023 Mar 6;e0198422.  [Abstract]

    MG-132 (200?nM; 24 h) significantly inhibits Newcastle disease virus (NDV) infection-caused degradation of β-catenin in DF-1 cells.

    MG-132 purchased from MCE. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107990.  [Abstract]

    PMs are treated with MG132 (10 μM). Endogenous YAP protein accumulated in the presence of MG132 starts from 2 h and further increases at 4 and 6 h after treatment in WT macrophages.

    MG-132 purchased from MCE. Usage Cited in: Brain Behav Immun. 2019 Jul;79:244-255.  [Abstract]

    Effect of autolysosome inhibitor (chloroquine, CQ, 50 μM) or proteasome inhibitor (MG132, 5 μM) on KA-induced NLRP3 degradation. Cells are treated with the inhibitors for 0.5 h before KA (10 μM, 2 h) treatment.

    MG-132 purchased from MCE. Usage Cited in: EMBO J. 2019 Mar 15;38(6):e100376.  [Abstract]

    Brcc3+/+ and Brcc3-/- (Abro1+/+ and Abro1-/-)BMDMs are treated with or without LPS for 1 h. Before LPS treatment, Brcc3-/- (Abro1-/-) BMDMs are pretreated with MG132 (10 μM) for 6 h to rescue the expression of ABRO1. Immunoblot analysis of NLRP3 and ABRO1 proteins in cell lysates immunoprecipitated with anti-ABRO1 antibody.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 26;38(1):101.  [Abstract]

    HLF and Hep3B cells are treated with Mg132 (10 μg/ml) for 4 h, total protein is extracted and subjected to western blotting using anti-Flag, anti-p21, or anti-GAPDH antibodies.

    MG-132 purchased from MCE. Usage Cited in: J Exp Bot. 2019 Sep 24;70(18):4749-4762.  [Abstract]

    Cell-free degradation assay of recombinant His-PhCHS protein. Recombinant His- PhCHS is purified from Escherichia coli incubated with petal crude proteins at stages and treated with specific 26S proteasome inhibitor MG132 at various time intervals. Western blot analysis was conducted using an anti-His antibody and anti-β-actin protein concentration was used as a loading control.

    MG-132 purchased from MCE. Usage Cited in: Antioxid Redox Signal. 2019 May 20;30(15):1831-1848.  [Abstract]

    Tan-IIA increases the endogenous induction of Nrf2 induction and this effect is further enhanced by cotreatment with the proteasome inhibitor MG-132.

    MG-132 purchased from MCE. Usage Cited in: Molecules. 2019 Jan 22;24(3):393.  [Abstract]

    The HepG2 cells are pretreated for 5 h MG 132 which is a proteasome inhibitor. Then, the MARCH1 protein expressions in HepG2 cells treated with 0 μM, 5,0 μM SAF, and 2.5 μM MG 132 are measured by immunoblotting.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 15;37(1):193.  [Abstract]

    Western blot is performed in HCC-LM3 cells transfected with HJURP knockdown lentivirus and treated with DMSO or MG132.

    MG-132 purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Oct 3;37(1):240.  [Abstract]

    Decrease of ERCC6 expression can be rescued with proteasome inhibitor MG132. Subconfluent SKOV3 cells are treated with FL118 and MG132 alone or in combination as shown for 8 h, followed by western blot analyses with ERCC6 antibody.

    MG-132 purchased from MCE. Usage Cited in: Cancer Res. 2019 Feb 1;79(3):534-545.  [Abstract]

    Cells are transfected with GYS2 siRNA and pre-incubated with MG-132 (20 μM) for 12 h. Cell lysate are immunoprecipitated by anti-Ub and immunoblotted by anti-p53.

    MG-132 purchased from MCE. Usage Cited in: EBioMedicine. 2018 Aug;34:243-255.  [Abstract]

    MPC1 protein expression in primary mouse hepatocytes incubated with pyruvate for 8 h in the presence of MG-132.

    MG-132 purchased from MCE. Usage Cited in: Cell Prolif. 2018 Aug;51(4):e12451.  [Abstract]

    Immunoblot analysis of CDK4 in cells treated with 4 μM of CGN for 24 hours in the presence and absence of MG132.

    MG-132 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 May 22;9(6):604.  [Abstract]

    Different concentrations of two classical proteasome inhibitors PS-341 and MG132 are added. AGS cells are either untreated or treated with PS-341 (25?nM) or MG132 (0.1?μM) for 24?h in the absence or presence of baf A1 (100?nM).

    MG-132 purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Feb 1;146:251-259.  [Abstract]

    In the absence of MG132, the protein degradation pathways are intact, the Tau protein level is significantly decreased in peptide 1-treated group.

    MG-132 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Apr 19;9:377.  [Abstract]

    Immunoblot levels of highly molecular weight (HMW)-ubiquitinated proteins and pSer129-α-syn after inhibiting the ubiquitin-proteasome system (UPS) by various concentrations of MG132 (0.25, 0.5, and 1 μM) in SH-SY5Y cells.

    MG-132 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2018 Oct;156:511-523.  [Abstract]

    The accumulated poly-ubiquitinated protein is detected by Western blotting after J-Lat 10.6 cells are treated with DMSO, PR-957 (100 nM), PR-957 (150 nM) or MG132 (500 nM) for 48 h.

    MG-132 purchased from MCE. Usage Cited in: Mol Plant Pathol. 2018 Dec;19(12):2623-2634.  [Abstract]

    Destabilization of BRC1 mediated by SWP1 is inhibited by proteasome inhibitors Epoxomicin and MG132.

    MG-132 purchased from MCE. Usage Cited in: Cell Cycle. 2018;17(13):1591-1601.  [Abstract]

    The protein level of CCNB1 in different groups is analyzed by Western blot; MG132 significantly increases the protein level of CCNB1 in oocytes from CRS group mice. Western blotting showing the reduced expression of securin is rescued by MG132 in CRS group mouse oocytes.

    MG-132 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78.  [Abstract]

    Western analysis of proteins expression with treatment of IKK-16 or MG-132.

    MG-132 purchased from MCE. Usage Cited in: Oncol Lett. 2018 Nov;16(5):5900-5906.  [Abstract]

    Treatment with the 26S proteasome inhibitor, MG 132 (10 μM), rescues the downregulation of NEK 8 in the pVHL overexpressing SGC 7901 cells.

    MG-132 purchased from MCE. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Oct;1864(10):3322-3338.  [Abstract]

    The neonatal rat cardiomyocytes (NRCMs) are treated with MG132 (10 μM). The protein expression level of PPARα in the indicated group.

    MG-132 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Dec 1;410:112-123.  [Abstract]

    Immunoprecipitation of ubiquitin from lysates of U-2 OS cells expressing CHOP after treatment with different concentrations of MG7 for 48 h. Cells are incubated with MG132 (20 mM) for 4 h before harvest. Cell lysates are immunoblotted with the indicated antibodies.

    MG-132 purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 7;7(1):2929.  [Abstract]

    p53 and Cell apoptosis. MCF7 and MDA-MB-231 cells are treated with 80?μM ω-3 FFAs, 20?μM ATRA alone or in combination for 48?h. The expression of PARP and p53 protein. β-Actin is used as an internal control.

    MG-132 purchased from MCE. Usage Cited in: J Inorg Biochem. 2017 Oct;175:92-100.  [Abstract]

    TPEN-triggered PML-RARα degradation in NB4 cells is reversed by MG-132 treatment. NB4 cells are treated with 5 μM TPEN with or without the presence of 1 μM MG-132 for the indicated durations (0–12 h) and then lysed. The lysates are analyzed for PML-RARα and RARα protein levels by western blotting.

    MG-132 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Sep 2;490(4):1168-1175.  [Abstract]

    Treatment of CHO-K1 cells with proteasome inhibitor, MG-132 results in elevated SR-B1 protein levels. The cells with MG-132, a potent proteasome inhibitor that inhibit ubiquitin/proteasome-dependent protein degradation, and MG-132 treatment significantly enhances cellular SR-B1 protein level.

    MG-132 purchased from MCE. Usage Cited in: Université de Montréal. Octobre 2017.

    Unsynchronized control and ARF6 cells are treated with DMSO or MG132 (10 μM) for 1h or 4h, lysed and total ubiquitinated proteins are determined using western blot (n=3).

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis[1][2][3].

    IC50 & Target

    IC50: 100 nM (Proteasome), 1.2 μM (Calpain)[1][3]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    COS-7 IC50
    < 10 μM
    Compound: MG132
    Cytotoxicity against african green monkey COS7 cells by XTT method
    Cytotoxicity against african green monkey COS7 cells by XTT method
    		[PMID: 18088097]
    HCT-116 IC50
    0.82 μM
    Compound: MG132
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    		[PMID: 31312413]
    HEK293 IC50
    0.009 μM
    Compound: MG132
    Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay
    Inhibition of chymotrypsin-like activity of proteasome beta-5 subunit in HEK293 cells using Suc-LLVY-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta5 assay
    		[PMID: 23540790]
    HEK293 IC50
    0.6 μM
    Compound: MG132
    Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay
    Inhibition of postacid activity of 20s proteasome beta-1 subunit in HEK293 cells using Z-nLPnLD-Glo as substrate incubated for 2 hrs prior to substrate addition measured after 10 mins by cell-based proteasome-Glo beta1 assay
    		[PMID: 23540790]
    Huh-7 IC50
    < 10 μM
    Compound: MG132
    Cytotoxicity against human HuH7 cells by XTT method
    Cytotoxicity against human HuH7 cells by XTT method
    		[PMID: 18088097]
    MCF-10A IC50
    0.29 μM
    Compound: MG-132
    Growth inhibition of human MCF10A cells after 72 hrs by CellTiter-Blue assay
    Growth inhibition of human MCF10A cells after 72 hrs by CellTiter-Blue assay
    		[PMID: 24153206]
    MCF7 IC50
    0.13 μM
    Compound: MG-132
    Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay
    Growth inhibition of human MCF7 cells after 72 hrs by CellTiter-Blue assay
    		[PMID: 24153206]
    MDA-MB-231 IC50
    0.18 μM
    Compound: MG-132
    Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay
    Growth inhibition of human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay
    		[PMID: 24153206]
    NCI-H23 IC50
    0.48 μM
    Compound: MG-132
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H23 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    NCI-H727 IC50
    0.98 μM
    Compound: MG-132
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    Cytotoxicity against human NCI-H727 cells after 72 hrs by CellTiter 96 AQueous one solution cell proliferation assay
    		[PMID: 30964987]
    NCI-H929 IC50
    0.17 μM
    Compound: MG-132
    Cytotoxicity against human NCI-H929 cells after 3 days by Alamar blue assay
    Cytotoxicity against human NCI-H929 cells after 3 days by Alamar blue assay
    		[PMID: 24625088]
    OCI-Ly3 IC50
    > 10 μM
    Compound: 1, MG-132
    Cytotoxicity against NF-kappaB overexpressing human OCI-Ly3 cells after 4 hrs
    Cytotoxicity against NF-kappaB overexpressing human OCI-Ly3 cells after 4 hrs
    		[PMID: 18024113]
    RAW264.7 IC50
    0.08 μg/mL
    Compound: MG132
    Inhibition of LPS and IFN-gamma-stimulated nitric oxide production in mouse RAW264.7 cells after 18 hrs by Griess method
    Inhibition of LPS and IFN-gamma-stimulated nitric oxide production in mouse RAW264.7 cells after 18 hrs by Griess method
    		[PMID: 26351042]
    RAW264.7 IC50
    0.08 μM
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent method
    		[PMID: 22620677]
    RAW264.7 IC50
    0.1 μM
    Compound: MG132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 18 hrs by Griess method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 18 hrs by Griess method
    		[PMID: 33422907]
    RAW264.7 IC50
    0.1 μM
    Compound: MG-132
    Inhibition of LPS-stimulated NO production in mouse RAW264.7 cells after 18 hrs by Griess assay
    Inhibition of LPS-stimulated NO production in mouse RAW264.7 cells after 18 hrs by Griess assay
    		[PMID: 24219809]
    RAW264.7 IC50
    0.1 μM
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess method
    		[PMID: 23819871]
    RAW264.7 IC50
    0.1 μM
    Compound: MG132
    Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells by Griess method
    Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells by Griess method
    		[PMID: 24597894]
    RAW264.7 IC50
    0.1 μM
    Compound: MG-132
    Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 18 hrs by griess reagent based plate reader analysis
    Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells after 18 hrs by griess reagent based plate reader analysis
    		[PMID: 24697496]
    RAW264.7 IC50
    0.15 μM
    Compound: MG-132
    Inhibition of LPS-induced NO production in mouse RAW264.7 cells at 25 uM preincubated with compound followed by LPS challenge measured after 18 hrs by Griess method
    Inhibition of LPS-induced NO production in mouse RAW264.7 cells at 25 uM preincubated with compound followed by LPS challenge measured after 18 hrs by Griess method
    		[PMID: 26757019]
    RAW264.7 IC50
    0.15 μM
    Compound: MG-132
    Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells measured after 18 hrs by Griess reagent based multilabel plate reader analysis
    Inhibition of nitric oxide production in LPS-stimulated mouse RAW264.7 cells measured after 18 hrs by Griess reagent based multilabel plate reader analysis
    		[PMID: 23327668]
    RAW264.7 IC50
    0.16 μM
    Compound: MG-132
    Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent based assay
    Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production after 18 hrs by Griess reagent based assay
    		[PMID: 30629435]
    RAW264.7 IC50
    0.17 μg/mL
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 5 mins by Greiss method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production after 5 mins by Greiss method
    		[PMID: 22277277]
    RAW264.7 IC50
    0.17 μg/mL
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-induced NO production after 5 mins by Greiss method
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFNgamma-induced NO production after 5 mins by Greiss method
    		[PMID: 22277277]
    RAW264.7 IC50
    0.18 μM
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess assay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by Griess assay
    		[PMID: 27203291]
    RAW264.7 IC50
    0.2 μM
    Compound: MG132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated iNOS activity preincubated with compound for 24 hrs followed by LPS stimulation for 2 hrs and measured 2 hrs after NADPH addition by fluorescence based assay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated iNOS activity preincubated with compound for 24 hrs followed by LPS stimulation for 2 hrs and measured 2 hrs after NADPH addition by fluorescence based assay
    		[PMID: 33454546]
    RAW264.7 IC50
    0.2 μM
    Compound: MG132
    Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells preincubated with compound for 24 hrs followed by LPS stimulation and measured after 2 hrs by Griess reagent-based assay
    Inhibition of NO production in LPS-stimulated mouse RAW264.7 cells preincubated with compound for 24 hrs followed by LPS stimulation and measured after 2 hrs by Griess reagent-based assay
    		[PMID: 33454546]
    RAW264.7 IC50
    0.2 μM
    Compound: MG-132
    Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production preincubated for 1 hr followed by LPS stimulation measured after 18 hrs by Griess assay
    Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production preincubated for 1 hr followed by LPS stimulation measured after 18 hrs by Griess assay
    		[PMID: 29338260]
    RAW264.7 IC50
    0.35 μM
    Compound: MG-132
    Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 18 hrs
    Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 18 hrs
    		[PMID: 21044847]
    RAW264.7 IC50
    0.35 μM
    Compound: MG-132
    Inhibition of NO production in Interferon gamma-stimulated mouse RAW264.7 cells after 18 hrs
    Inhibition of NO production in Interferon gamma-stimulated mouse RAW264.7 cells after 18 hrs
    		[PMID: 21044847]
    RAW264.7 IC50
    0.63 μM
    Compound: MG132
    Toxicity against mouse RAW264.7 cells by XTT assay
    Toxicity against mouse RAW264.7 cells by XTT assay
    		[PMID: 22858297]
    RAW264.7 IC50
    2.6 μM
    Compound: MG132
    Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated with compound for 2 hrs followed by LPS stimulation for 12 hrs by Griess reagent based analysis
    Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production pretreated with compound for 2 hrs followed by LPS stimulation for 12 hrs by Griess reagent based analysis
    		[PMID: 36607819]
    SW480 IC50
    29.5 μM
    Compound: MG132
    Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay
    Inhibition of NFkappaB transcription in human SW480 cells at by luciferase reporter gene assay
    		[PMID: 26841168]
    體外研究
    (In Vitro)

    MG-132 (Z-Leu-Leu-Leu-al) 在低濃度 (30 nM) 下啟動(dòng) PC12 細(xì)胞的神經(jīng)突生長(zhǎng)，是一種非常強(qiáng)的 20S 蛋白酶體抑制劑[3]。
    MG-132 (10 μM；1 小時(shí)) 可逆轉(zhuǎn) A549 細(xì)胞中 TNF-α 對(duì) IκB 降解和 NF-κ B 活化的影響[4]。
    MG- 132 (0.75-5 μM；24 小時(shí)) 通過(guò) 26S 蛋白酶體抑制作用在 KIM-2 細(xì)胞中有效誘導(dǎo) p53 依賴(lài)性細(xì)胞凋亡[5]。
    MG-132 (10-40 μM；24小時(shí)) 以時(shí)間依賴(lài)性和濃度依賴(lài)性方式顯著降低 C6 神經(jīng)膠質(zhì)瘤細(xì)胞的活力，并顯示 IC50 在 24 小時(shí)時(shí)為 18.5 μM[6]。
    MG-132 (18.5 μM；24 小時(shí)) 誘導(dǎo)抗凋亡蛋白 Bcl-2 和 XIAP 的下調(diào)，并上調(diào)促凋亡蛋白 Bax 和 caspase-3 的表達(dá)[6]。

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

    Cell Viability Assay[3]

    Cell Line: C6 glioma cells
    Concentration: 10, 20, 30, 40 μM
    Incubation Time: 24 hours
    Result: Significantly reduced the viability of C6 glioma cells beginning at 6 h in both time- and concentration-dependent manners and showed the IC50 of 18.5 μM at 24 hours.

    Western Blot Analysis[3]

    Cell Line: A549 cells
    Concentration: 10 μM
    Incubation Time: 1 hour
    Result: Reversed the effects of TNF-α on IκB degradation and resulted in a reversal of TNF-α-induced NF-κB activation.
    體內(nèi)研究
    (In Vivo)

    MG-132 (10 mg/kg；腹腔注射；從注射 EC9706 細(xì)胞后 5 天開(kāi)始每天施用 25 天) 顯著抑制 EC9706 異種移植物的腫瘤生長(zhǎng)，而不會(huì)對(duì)小鼠造成毒性[7]。
    MG-132 (1 mg/kg；靜脈注射；每周兩次，持續(xù) 4 周) 對(duì)攜帶 HeLa 腫瘤的小鼠顯示出有效的腫瘤抑制作用[8]。
    MG-132 (1-10 μg/kg/day；皮下植入滲透泵；持續(xù) 8 天) 顯著增加小鼠骨骼肌裂解液中 β-肌營(yíng)養(yǎng)不良聚糖、α-肌營(yíng)養(yǎng)不良聚糖、α-肌肌聚糖和抗肌萎縮蛋白的表達(dá)水平 (6 月齡雄性 C57BL/10ScSn DMD mdx 小鼠)[9]。

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

    Animal Model: 5- to 6-weeks old female athymic nude mice (EC9706 xenograft)
    Dosage: 10 mg/kg
    Administration: I.p.; daily for 25 days starting 5 days after EC9706 cells injection
    Result: Significantly inhibited tumor growth of the EC9706 xenograft without causing toxicity to the mice.
    Animal Model: Five-week-old female C.B-17/lcr-scid/scidJcl mice (bearing HeLa cells)[8]
    Dosage: 1 mg/kg
    Administration: Intravenous injection; twice a week for 4 weeks
    Result: The growth inhibition rates in HeLa tumors was 49% compared to the control.
    分子量

    475.62

    Formula

    C26H41N3O5
    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
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 100 mg/mL (210.25 mM; 超聲助溶; 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)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 2.1025 mL 10.5126 mL 21.0252 mL
    5 mM 0.4205 mL 2.1025 mL 4.2050 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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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: ≥ 1.67 mg/mL (3.51 mM); 澄清溶液

      此方案可獲得 ≥ 1.67 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 16.7 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: 1.67 mg/mL (3.51 mM); 懸濁液; 超聲助溶

      此方案可獲得 1.67 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 16.7 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。
    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: 99.97%

    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, 6 months; -20°C, 1 month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)月內(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 2.1025 mL 10.5126 mL 21.0252 mL 52.5630 mL
    5 mM 0.4205 mL 2.1025 mL 4.2050 mL 10.5126 mL
    10 mM 0.2103 mL 1.0513 mL 2.1025 mL 5.2563 mL
    15 mM 0.1402 mL 0.7008 mL 1.4017 mL 3.5042 mL
    20 mM 0.1051 mL 0.5256 mL 1.0513 mL 2.6281 mL
    25 mM 0.0841 mL 0.4205 mL 0.8410 mL 2.1025 mL
    30 mM 0.0701 mL 0.3504 mL 0.7008 mL 1.7521 mL
    40 mM 0.0526 mL 0.2628 mL 0.5256 mL 1.3141 mL
    50 mM 0.0421 mL 0.2103 mL 0.4205 mL 1.0513 mL
    60 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8760 mL
    80 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6570 mL
    100 mM 0.0210 mL 0.1051 mL 0.2103 mL 0.5256 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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