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  2. MAPK/ERK Pathway Autophagy Apoptosis
  3. JNK Autophagy Apoptosis Ferroptosis
  4. SP600125

SP600125 是一種口服有效的，可逆的，ATP競爭性的 JNK 抑制劑，抑制 JNK1， JNK2 和 JNK3 的 IC50 分別為 40，40，90 nM。SP600125 是一種有效的鐵死亡 (ferroptosis) 抑制劑。SP600125 能誘導(dǎo)膀胱癌細胞自噬 (autophagy) 向凋亡 (apoptosis) 的轉(zhuǎn)化。

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

SP600125 Chemical Structure

SP600125 Chemical Structure

CAS No. : 129-56-6

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥605
In-stock
5 mg ￥343
In-stock
10 mg ￥550
In-stock
50 mg ￥850
In-stock
100 mg ￥1250
In-stock
200 mg ￥2250
In-stock
500 mg ￥4800
In-stock
1 g   詢價  
5 g   詢價  

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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 478 篇科研文獻

WB
RT-PCR

    SP600125 purchased from MCE. Usage Cited in: Cytotherapy. 2023 Mar 6;S1465-3249(23)00037-3.  [Abstract]

    SP600125 (10 μM; 24 h) decreases the protein levels of p-JNK and p-c-Jun in THP-1 and U937 cells.

    SP600125 purchased from MCE. Usage Cited in: Exp Neurol. 2020 Sep;331:113374.  [Abstract]

    Effects of SP600125 attenuated p-JNK and RIPK3-mediated necroptosis after I/R injury. Representative western blot images and quantification of the protein expression of p-JNK, IL-6, pRIPK3 and AIF in the group pretreated with SP600125 before I/R.

    SP600125 purchased from MCE. Usage Cited in: Chem Biol Interact. 2019 Sep 1;310:108748.  [Abstract]

    Followed by 10 μM SP600125 incubation for 3 or 6 h, the protein levels of t-JNK, p-JNK, t-c-Jun and p-c-Jun in MC3T3-E1 cells are detected by western blotting.

    SP600125 purchased from MCE. Usage Cited in: J Cell Biochem. 2019 Mar;120(3):3898-3910.  [Abstract]

    Cells pretreated with SP600125 show a decreased proapoptotic Bax expression and increase antiapoptotic Bcl-2 formation when JNK pathway is blocked. Inhibition of p38 by SB202190 significantly enhanced Bcl-2 expression. Pretreatment with BAY 11-7082 to inhibit NF‐κB markedly enhance Baxm and decrease Bcl-2 expression compared with the ACR-treated group.

    SP600125 purchased from MCE. Usage Cited in: Acta Biochim Biophys Sin (Shanghai). 2019 Apr 1;51(4):365-374.  [Abstract]

    MAPKs inhibitors suppress LPS-induced COX-2 expression and AKT1 phosphorylation. RAW264.7 cells are pretreated for 1 h with U0126, SB202190, SP600125 alone, or all the three inhibitors, respectively, and then exposed to 40 ng/ml LPS for 30 min or 12 h. The phosphorylated protein kinases and COX-2 expression are detected by western blot analysis using their corresponding antibodies.

    SP600125 purchased from MCE. Usage Cited in: J Autoimmun. 2018 May;89:30-40.  [Abstract]

    The protein expression of S100A7 in keratinocytes incubated with DMSO or JNK inhibitor SP600125 for 48 h after transfection with siRNA for 24 h.

    SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Oct 19;15(1):291.  [Abstract]

    Blocking the three MAPK signaling pathways through specific inhibitors (U0126; SB202190; and SP600125) significantly decrease the infection-induced neuroinflammatory response via real-time PCR analysis.

    SP600125 purchased from MCE. Usage Cited in: J Neuroinflammation. 2018 Jun 15;15(1):184.  [Abstract]

    Representative immunoblots of total lysates from BV2 cells treated with MPP+or/and U0126 (10 μM), SP600125 (SP, 10 μM) and SB203580 (SB, 10 μM) using the antibodies against DICER.

    SP600125 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Mar;75(6):1117-1132.  [Abstract]

    Sertoli cells (SC) are pretreated with the SP600125 for 1 h followed by a 24-h treatment with MC-LR. Expression levels of MMP-8, c-Jun, c-Fos, p-ERK, ERK, p-JNK, and JNK are determined by western blotting.

    SP600125 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2018 Jul;75(14):2627-2641.  [Abstract]

    RAW264.7 macrophages are pre-treated with the inhibitor of ERK, JNK, P38, P65, and AKT signal pathway.Western blot analyzes the non- and phosphorylation of ERK, JNK, P38, P65, and AKT.

    SP600125 purchased from MCE. Usage Cited in: Phytomedicine. 2018 Mar 15;42:152-163.  [Abstract]

    Cells are pretreated with SP600125 (20 μM), SB203580 (20 μM) or U0126 (20 μM) in presence or absence of KLA, then incubated with LPS (1 μg/mL) for certain time. Cell lysates are subjected to western blot.

    SP600125 purchased from MCE. Usage Cited in: Free Radic Biol Med. 2018 Jun 2;124:205-213.  [Abstract]

    Total and phosphorylation levels of JNK in MCF7 and MDAMB231 after SP600125 treatment at 24 h.

    SP600125 purchased from MCE. Usage Cited in: Br J Pharmacol. 2018 Dec;175(23):4338-4352.  [Abstract]

    Treatment of macrophages with inhibitor of p38 (SB203580) or JNK (SP600125) inhibits the synthesis of pro-IL-1β in ZFP91-overexpressing THP-1 cells.

    SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein levels of IL-1β and TNF-α are sharply downregulated by the addition of inhibitors SB203580, SP600125, and U0126.

    SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-ERK1/2/ERK1/2 is notably reduced by inhibitors SB203580, SP600125, and U0126.

    SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    The protein level of MMP-9 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-JNK1&JNK1 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SP600125 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2018 Oct 3;108:1294-1302.  [Abstract]

    As for both 0 g and 3 g groups, the p-p38&p38 is downregulated by inhibitors SB203580, SP600125, and U0126.

    SP600125 purchased from MCE. Usage Cited in: J Agric Food Chem. 2018 Jun 27;66(25):6317-6325.  [Abstract]

    HepG2 cells are pre-incubated with 20 μM SB203580, SP600125 and PD98059 for 1 h and then treated with tangeretin(20μM) for 24 h.

    SP600125 purchased from MCE. Usage Cited in: FASEB J. 2018 May;32(5):2722-2734.  [Abstract]

    Cultured L02 cells exposed to 1% BSA or 200 mM PA for 12 h are pretreated with JNK inhibitor (SP600125) for 2 h. Intracellular and released HMGB1 are analyzed.

    SP600125 purchased from MCE. Usage Cited in: Sci Rep. 2018 Apr 23;8(1):6379.  [Abstract]

    Immunoblot analysis of lysates from Anisomycin pre-treatment cells reveals an increase of CHIP protein compared with OGD treated only cells, contrasting with a decrease in RIPK3 and p-MLKL protei. Pre-treatment cells with SP600125 results in the expected attenuation in JNK phosphorylation levels.

    SP600125 purchased from MCE. Usage Cited in: Onco Targets Ther. 2018 Nov 28;11:8435-8444.  [Abstract]

    Western blot results of active caspase 3 and JNK pathway-related genes in the treatment of CON, XRCC1-ON and SP600125.

    SP600125 purchased from MCE. Usage Cited in: J Mol Endocrinol. 2018 Feb;60(2):145-157.  [Abstract]

    SP600125 decreases Keap1 expression through inhibition of JNK activity.

    SP600125 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Sep 5;503(2):903-909.  [Abstract]

    Inactivation of JNK using SP600125 in the PTP1B overexpressing cancer cells largely restores the expression levels of Twist, vimentin and Ecadherin.

    SP600125 purchased from MCE. Usage Cited in: bioRxiv. August 2, 2018.

    AGS-EBV and B95.8 cells are pretreated with SP600125 (0, 50, and 100 nM) for 24. Equal amounts of cell lysates are prepared and western blot analysis is performed to determine the levels of total and phosphorylated ERKs, p38, and JNKs and EBV lytic proteins.

    SP600125 purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2018;46(5):1779-1792.  [Abstract]

    Western blot bands of p38, phospho-p38, ZO-1, Clau-din-1, and Occludin. JNK inhibitor SP600125 and p38 inhibitor SB203580 are used.

    SP600125 purchased from MCE. Usage Cited in: Cell Death Differ. 2017 Mar;24(3):492-499.  [Abstract]

    LPS stimulates ICER expression via p38-CREB pathway. Effect of MAPK and IKK inhibitors on LPS-induced CREB phosphorylation in peritoneal macrophages.

    SP600125 purchased from MCE. Usage Cited in: Cancer Lett. 2017 Feb 16;393:22-32.  [Abstract]

    Effects of p38 MAPK inhibitor (SB203580), ERK inhibitor (U0126), JNK inhibitor (SP600125), caspase inhibitor (Z-VAD-FMK) and NAC on SGC-7901 and MGC-803 treated with DOX/VCPA combination treatment. VCPA pretreatment strategy is the same as above. SB203580 (20 μM), U0126 (10 μM), SP600125 (20 μM), Z-VAD-FMK (10 μM) and NAC (5 mM) are treated 2 h before DOX (2 μg/mL) added into the culture, respectively. MAPK pathway protein levels are determined.

    SP600125 purchased from MCE. Usage Cited in: Oncoimmunology. 2017 Dec 26;7(4):e1412910.  [Abstract]

    The down-regulated phosphorylation of SAPK/JNK pathway by 10μM SP600125 is detected in RAW264.7 by Western blot. The down-regulated phosphorylation of SAPK/JNK pathway by 15mg/kg SP600125 is detected in peritoneal macrophages in vivo by Western blot.

    SP600125 purchased from MCE. Usage Cited in: Int J Mol Med. 2017 Jan;39(1):71-80.  [Abstract]

    Inhibition of c-Jun N-terminal kinase (JNK) expression enhances the promoting effects of miR-214 on adipocyte differentiation and decreases p-JNK protein expression in bone marrow-derived mesenchymal stem cells (BMSCs) following the overexpression of miR-214. p-JNK protein expression is even more significantly suppressed by treatment of the cells with JNK inhibitor as shown by (A) western blot analysis and (B) statistical analysis of p-JNK protein expression.

    SP600125 purchased from MCE. Usage Cited in: Chem Biol Interact. 2017 Nov 1;277:62-73.  [Abstract]

    Effects of silencing p53 on colistin-induced ROS production and p-JNK expression level in PC-12 cells. The protein levels of p53. The protein levels of p-JNK by western blot.

    SP600125 purchased from MCE. Usage Cited in: Mol Immunol. 2017 Jul;87:161-170.  [Abstract]

    Effect of TLR2 on autophagy activation via ERK signaling pathway in MG-infected RAW264.7 cells. RAW264.7 cells transfected with TLR2 siRNA/control siRNA are infected with MG for 30 min prior to SP600125. The expression levels of Beclin1, LC3-II/I, p-JNK, p-ERK1/2 and p-p38 are examined by Western blot. The GAPDH level was used as the internal standard.

    SP600125 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7426458.  [Abstract]

    Representative immunoblot analysis of p53, p16, p21, and retinoblastoma protein (Rb) in NP cells.

    SP600125 purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:6175841.  [Abstract]

    Involvements of MAPK signaling pathway in CPS-induced apoptosis in ALI cultures of sheep bronchial epithelial cells. Cells are pretreated with SP600125 (a JNK inhibitor, 20?μM) for 1?h, followed by exposure to CPS (100?ng/mL) or MO (MOI = 30) for 48?h. Cell lysates are subjected to Western blotting analysis using indicated antibodies.

    SP600125 purchased from MCE. Usage Cited in: Oncotarget. 2016 Dec 20;7(51):85079-85096.  [Abstract]

    IL-37b inhibits TNF-α mediated activation of the pSmad3L/c-myc pathway but potentiates pSmad3C/ p21 expression in SMMC-7721 cells. Serum-starved LV_NC and LV_IL1F7b-infected SMMC-7721 cells are incubated for 8 h in the absence or presence of 10 μM SP600125 and are then treated for 30 mins with 400 pM TNF-α. Expression of endogenous Smad3 phosphorylation, p21, and c-myc is analyzed in Western blot using specific Abs.

    SP600125 purchased from MCE. Usage Cited in: J Mol Cell Cardiol. 2015 Dec;89(Pt B):268-79.  [Abstract]

    Dose response of MAPK and Akt inhibitors on cardiac fibroblast-derived exosomes (Exo)-induced activation of MAPKs and Akt. Neonatal rat cardiomyocytes are treated with or without Exo (50 μg/mL), U0126, SP600125, MK-2206, and SB023580 for 20 min and subjected to Western blot analysis. The results are from 4 separate experiments.

    查看 JNK 亞型特異性產(chǎn)品:

    • 生物活性

    • 實驗參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻

    生物活性

    SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis[1][2][3].

    IC50 & Target[1]

    JNK1

    40 nM (IC50)

    JNK2

    40 nM (IC50)

    JNK3

    90 nM (IC50)

    Autophagy

     

    細胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    786-0 IC50
    27.1 μM
    Compound: SP600125
    Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human 786-0 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    A498 IC50
    7.03 μM
    Compound: SP600125
    Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human A498 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    A549 IC50
    14.93 μM
    Compound: SP600125
    Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human A549 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    ACHN IC50
    6.64 μM
    Compound: SP600125
    Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human ACHN cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    BT-549 IC50
    30.76 μM
    Compound: SP600125
    Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human BT-549 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    CAKI-1 IC50
    3.56 μM
    Compound: SP600125
    Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human CAKI-1 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    CCRF-CEM IC50
    16.03 μM
    Compound: SP600125
    Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human CCRF-CEM cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    COLO 205 IC50
    19.54 μM
    Compound: SP600125
    Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human COLO 205 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    DU-145 IC50
    28.18 μM
    Compound: SP600125
    Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human DU-145 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    EKVX IC50
    20.04 μM
    Compound: SP600125
    Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human EKVX cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HCC 2998 IC50
    9.62 μM
    Compound: SP600125
    Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HCC 2998 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HCT-116 IC50
    44.57 μM
    Compound: SP600125
    Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HCT-116 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HCT-15 IC50
    8.04 μM
    Compound: SP600125
    Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HCT-15 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HL-60(TB) IC50
    42.07 μM
    Compound: SP600125
    Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HL-60(TB) cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HOP-62 IC50
    69.34 μM
    Compound: SP600125
    Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HOP-62 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HOP-92 IC50
    37.58 μM
    Compound: SP600125
    Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HOP-92 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    Hs-578T IC50
    55.08 μM
    Compound: SP600125
    Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human Hs-578T cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    HT-29 IC50
    25.88 μM
    Compound: SP600125
    Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human HT-29 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    IGROV-1 IC50
    11.35 μM
    Compound: SP600125
    Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human IGROV-1 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    K562 IC50
    48.64 μM
    Compound: SP600125
    Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human K562 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    KM12 IC50
    2.62 μM
    Compound: SP600125
    Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human KM12 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    M14 IC50
    > 100 μM
    Compound: SP600125
    Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human M14 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    Malme-3M IC50
    16.41 μM
    Compound: SP600125
    Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human Malme-3M cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    MCF7 IC50
    48.98 μM
    Compound: SP600125
    Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human MCF7 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    MDA-MB-231 IC50
    65.31 μM
    Compound: SP600125
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    MDA-MB-435 IC50
    12.82 μM
    Compound: SP600125
    Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-435 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    MOLT-4 IC50
    20.37 μM
    Compound: SP600125
    Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human MOLT-4 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    MONO-MAC-6 IC50
    5.2 μM
    Compound: SP600125
    Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
    Inhibition of JNK in human MONO-MAC-6 cells assessed as reduction in LPS-induced IL6 production preincubated for 30 mins followed by LPS-stimulation and measured after 24 hrs by ELISA
    		[PMID: 30347329]
    NCI/ADR-RES IC50
    22.59 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-ADR-RES cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    NCI-H226 IC50
    22.86 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H226 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    NCI-H23 IC50
    23.77 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H23 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    NCI-H322M IC50
    24.95 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H322M cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    NCI-H460 IC50
    9.86 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H460 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    NCI-H522 IC50
    12.19 μM
    Compound: SP600125
    Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human NCI-H522 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    OVCAR-3 IC50
    15.31 μM
    Compound: SP600125
    Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human OVCAR-3 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    OVCAR-4 IC50
    31.91 μM
    Compound: SP600125
    Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human OVCAR-4 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    OVCAR-5 IC50
    24.38 μM
    Compound: SP600125
    Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human OVCAR-5 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    OVCAR-8 IC50
    22.03 μM
    Compound: SP600125
    Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human OVCAR-8 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    PC-3 IC50
    23.28 μM
    Compound: SP600125
    Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human PC-3 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    RPMI-8226 IC50
    18.79 μM
    Compound: SP600125
    Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human RPMI-8226 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    RXF 393 IC50
    20.75 μM
    Compound: SP600125
    Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human RXF 393 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SF-268 IC50
    18.45 μM
    Compound: SP600125
    Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SF-268 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SF-295 IC50
    22.49 μM
    Compound: SP600125
    Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SF-295 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SF-539 IC50
    32.21 μM
    Compound: SP600125
    Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SF-539 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SK-MEL-2 IC50
    28.97 μM
    Compound: SP600125
    Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SK-MEL-2 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SK-MEL-28 IC50
    37.5 μM
    Compound: SP600125
    Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SK-MEL-28 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SK-MEL-5 IC50
    14.62 μM
    Compound: SP600125
    Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SK-MEL-5 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SK-OV-3 IC50
    20.99 μM
    Compound: SP600125
    Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SK-OV-3 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SN12C IC50
    14.76 μM
    Compound: SP600125
    Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SN12C cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SNB-19 IC50
    50 μM
    Compound: SP600125
    Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SNB-19 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SNB-75 IC50
    16.9 μM
    Compound: SP600125
    Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SNB-75 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SR IC50
    13.09 μM
    Compound: SP600125
    Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SR cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    SW-620 IC50
    10.91 μM
    Compound: SP600125
    Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human SW-620 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    T47D IC50
    > 100 μM
    Compound: SP600125
    Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human T47D cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    TK-10 IC50
    5.93 μM
    Compound: SP600125
    Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human TK-10 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    U-251 IC50
    23.07 μM
    Compound: SP600125
    Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human U-251 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    UACC-257 IC50
    29.51 μM
    Compound: SP600125
    Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human UACC-257 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    UACC-62 IC50
    14.55 μM
    Compound: SP600125
    Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human UACC-62 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    UO-31 IC50
    10.54 μM
    Compound: SP600125
    Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay
    Antiproliferative activity against human UO-31 cells measured after 48 hrs by SRB assay
    		[PMID: 35764033]
    WI-38 IC50
    > 20 μM
    Compound: SP600125
    Antiproliferative activity against human WI-38 cells measured by MTT assay
    Antiproliferative activity against human WI-38 cells measured by MTT assay
    		[PMID: 35764033]
    體外研究
    (In Vitro)

    SP600125 是 JNK2 的 ATP 競爭性抑制劑，Ki 值為 0.19±0.06 μM。SP600125 在 Jurkat T 細胞中抑制 c-Jun 的磷酸化，IC50 為 5 μM 至 10 μM。在 CD4+ 細胞中，例如從人臍帶血或外周血中分離的 Th0 細胞，SP600125 阻斷細胞活化和分化并抑制炎癥基因 COX-2、IL-2、IL-10、IFN-γ 和 TNF-α，IC50 為 5 μM 至 12 μM[1]。
    在小鼠 β 細胞 MIN6 中，SP600125 (20 μM) 誘導(dǎo) p38 MAPK 的磷酸化及其下游 CREB 依賴性啟動子激活[2]。
    在 HCT116 細胞中，SP600125 (20 μM) 阻斷 G2 期到有絲分裂的轉(zhuǎn)變并誘導(dǎo)核內(nèi)復(fù)制。SP600125 的這種能力獨立于 JNK 抑制，但由于其抑制 Aurora A 和 Polo 樣激酶 1 上游的 CDK1-細胞周期蛋白 B 激活[3]。

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

    SP600125 (15 mg/kg 或 30 mg/kg；靜脈注射) 顯著抑制 TNF-α 血清水平，而 30 mg/kg 口服施用后，則劑量依賴性地阻斷 TNF-α 表達[1]。
    SP600125 在大鼠體內(nèi)減輕 LPS 誘導(dǎo)的 ALI。SP600125 組大鼠 BALF 中 TNF-α和 IL-6 的表達水平顯著降低[4]。

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

    220.23

    Formula

    C14H8N2O
    CAS 號
    性狀

    固體

    顏色

    Yellow to green

    運輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細胞實驗： 

    DMSO 中的溶解度 : 12.5 mg/mL (56.76 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

    配制儲備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 4.5407 mL 22.7035 mL 45.4071 mL
    5 mM 0.9081 mL 4.5407 mL 9.0814 mL
    查看完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(nèi)使用。

    • 摩爾計算器

    • 稀釋計算器

    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

    動物實驗：

    請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (9.44 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 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 20.8 mg/mL 的澄清 DMSO 儲備液加到 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。

    以下溶解方案，請直接配制工作液。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； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請依序添加每種溶劑： Corn Oil

      Solubility: 1 mg/mL (4.54 mM); 懸濁液; 超聲助溶 (<80°C)

    • 方案 二

      請依序添加每種溶劑： 1% CMC-Na/saline water

      Solubility: 3.33 mg/mL (15.12 mM); 懸濁液; 超聲助溶

    動物溶解方案計算器
    請輸入動物實驗的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實驗過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲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: 99.73%

    參考文獻
    Cell Assay
    [1]

    Determination of mRNA half-life is performed essentially, except that CD14+ cells are stimulated with (bacterial) lipopolysaccharide (LPS; 50 ng/mL) for 2 h before addition of actinomycin D (5 μg/mL). SP600125 (25 μM) or vehicle (0.5% DMSO vol/vol) is added immediately following the actinomycin D. Analysis is performed by using real-time reverse transcription (RT)-PCR. Total RNA is extracted with an RNeasy Mini kit. TNF mRNA is measured by real time RT-PCR, using a TNF Taqman probe. All data are normalized by using glyceraldehyde-3-phosphate dehydrogenase (GAPDH) expression. The TNF-α forward primer is 5′-CTGGCCCAGGCAGTCAGAT-3′ and the reverse primer is 5′-TATCTCTCAGCTCCACGCCATT-3′. The Taqman probe sequence is 5′-FAM-CCTGTAGCCCATGTTGTAGCAAACCCTCA-TAMRA-3′[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][4]

    Mice[1]
    Female CD-1 mice (8-10 weeks of age) are dosed i.v. or per oswith SP600125 in PPCES vehicle (30% PEG-400/20% polypropylene glycol/15% Cremophor EL/5% ethanol/30% saline), final volume of 5 mL/kg, 15 min before i.v. injection with LPS in saline (0.5 mg/kg). At 90 min, a terminal bleed is obtained from the abdominal vena cava, and the serum is recovered. Samples are analyzed for mouse TNF-α by using an ELISA.
    Rats[4]
    A total of 40 male Wistar rats are randomly divided into four groups (n=10): the control group, LPS group, normal saline group (NS) and the SP600125 group. Acute lung injury (ALI) is induced via intratracheal injection of LPS. Normal saline or SP600125 is administered via intraperitoneal injection (15 mg/kg) 10 min after the LPS injection.

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

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內(nèi)使用， -20°C儲存時，請在1年內(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 4.5407 mL 22.7035 mL 45.4071 mL 113.5177 mL
    5 mM 0.9081 mL 4.5407 mL 9.0814 mL 22.7035 mL
    10 mM 0.4541 mL 2.2704 mL 4.5407 mL 11.3518 mL
    15 mM 0.3027 mL 1.5136 mL 3.0271 mL 7.5678 mL
    20 mM 0.2270 mL 1.1352 mL 2.2704 mL 5.6759 mL
    25 mM 0.1816 mL 0.9081 mL 1.8163 mL 4.5407 mL
    30 mM 0.1514 mL 0.7568 mL 1.5136 mL 3.7839 mL
    40 mM 0.1135 mL 0.5676 mL 1.1352 mL 2.8379 mL
    50 mM 0.0908 mL 0.4541 mL 0.9081 mL 2.2704 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：
    SP600125
    目錄號：
    HY-12041
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