SP600125 [129-56-6]

Cat# HY-12041-10mg

Size : 10mg

Brand : MedChemExpress

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SP600125 est un inhibiteur de JNK qui est actif par voie orale, réversible et ATP-compétitif avec des IC50 de 40, 40 et 90 nM pour JNK1, JNK2 et JNK3, respectivement. SP600125 est un inhibiteur puissant de la ferroptose. SP600125 inhibe l'autophagie et active l'apoptose.

SP600125 ist ein oral aktiver, reversibler und ATP-kompetitiver JNK-Inhibitor mit IC50s von 40, 40 und 90 nM für JNK1, JNK2 und JNK3. SP600125 ist ein potenter ferroptosis-Inhibitor. SP600125 hemmt die autophagy und aktiviert die apoptosis.

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.

For research use only. We do not sell to patients.

SP600125 Chemical Structure

SP600125 Chemical Structure

CAS No. : 129-56-6

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Based on 499 publication(s) in Google Scholar

    SP600125 purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.
    Description

    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

     

    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]
    In Vitro

    SP600125 is an ATP-competitive inhibitor of JNK2 with a Ki value of 0.19±0.06 μM. SP600125 inhibits the phosphorylation of c-Jun with IC50 of 5 μM to 10 μM in Jurkat T cells. In CD4+ cells, such as Th0 cells isolated from either human cord or peripheral blood, SP600125 blocks cell activation and differentiation and inhibits the expression of inflammatory genes COX-2, IL-2, IL-10, IFN-γ, and TNF-α, with IC50 of 5 μM to 12 μM[1].
    In a mouse beta cells MIN6, SP600125 (20 μM) induces the phosphorylation of p38 MAPK and its downstream CREB-dependent promoter activation[2].
    In HCT116 cells, SP600125 (20 μM) blocks the G2 phase to mitosis transition and induces endoreplication. This ability of SP600125 is independent of JNK inhibition, but due to its inhibition of CDK1-cyclin B activation upstream of Aurora A and Polo-like kinase 1[3].

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (56.76 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  Corn Oil

      Solubility: 1 mg/mL (4.54 mM); Suspended solution; Need ultrasonic and warming and heat to 80°C

    • Protocol 2

      Add each solvent one by one:  1% CMC-Na/saline water

      Solubility: 3.33 mg/mL (15.12 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.73%

    References
    • [1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686.  [Content Brief]

      [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860.  [Content Brief]

      [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716.  [Content Brief]

      [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158.  [Content Brief]

      [5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157.  [Content Brief]

      [6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43.  [Content Brief]

    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.

    References
    • [1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686.  [Content Brief]

      [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860.  [Content Brief]

      [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716.  [Content Brief]

      [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158.  [Content Brief]

      [5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157.  [Content Brief]

      [6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43.  [Content Brief]

    • [1]. Bennett BL, et al. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc Natl Acad Sci U S A, 2001, 98(24), 13681-13686.

      [2]. Vaishnav D, et al. SP600125, an inhibitor of c-jun N-terminal kinase, activates CREB by a p38 MAPK-mediated pathway. Biochem Biophys Res Commun, 2003, 307(4), 855-860.

      [3]. Kim JA, et al. SP600125 suppresses Cdk1 and induces endoreplication directly from G2 phase, independent of JNK inhibition. Oncogene, 2010, 29(11), 1702-1716.

      [4]. Zheng Y, et al. JNK inhibitor SP600125 protects against lipopolysaccharide-induced acute lung injury via upregulation ofclaudin-4. Exp Ther Med. 2014 Jul;8(1):153-158.

      [5]. Zhang H, et al. SP600125 Suppresses Keap1 Expression and Results in NRF2-mediated Prevention of Diabetic Nephropathy. J Mol Endocrinol. J Mol Endocrinol. 2018 Feb;60(2):145-157.

      [6]. Yatsushige H, et al. Role of c-Jun N-terminal kinase in cerebral vasospasm after experimental subarachnoid hemorrhage. Stroke. 2005 Jul;36(7):1538-43.

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 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
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    SP600125 Related Classifications

    • MAPK/ERK Pathway Autophagy Apoptosis
    • JNK Autophagy Apoptosis Ferroptosis
    Help & FAQs
    • Keywords:

      SP600125129-56-6SP 600125SP-600125JNKAutophagyApoptosisFerroptosisc-Jun N-terminal kinasereversibleATP-competitivephosphorylationInhibitorinhibitorinhibit

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