SP 600125

Cat. No. 1496

SP 600125 C14H8N2O [129-56-6]

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Chemical Name: Anthra[1-9-cd]pyrazol-6(2H)-one

Biological Activity

Selective JNK inhibitor. Competitively and reversibly inhibits JNK1, 2 and 3 (IC50 = 40 - 90 nM) with negligible activity at ERK2, p38β and a range of enzymes. Active in vivo. Exhibits reduced selectivity over other protein kinases under certain conditions. Protects renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis. Prevents BMP9-induced osteogenic differentiation of MSCs. Essential component of medium for maintaining stem cells in naive pluripotent state. Available as part of the MAPK Inhibitor Tocriset™.

Technical Data

Soluble to 5 mM in ethanol with gentle warming and to 100 mM in DMSO
>98 %
Desiccate at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Safety Data Sheet: View Safety Data Sheet

Gafni et al (2013) Derivation of novel human ground state naive pluripotent stem cells. Nature 504 282. PMID: 24172903.

Zhao et al (2013) Activation of JNKs is essential for BMP9-induced osteogenic differentiation of mesenchymal stem cells. BMB Rep. 46 422. PMID: 23977991.

Wang et al (2007) SP600125, a selective JNK inhibitor, protects ischemic renal injury via suppressing the extrinsic pathways of apoptosis. Life Sci. 80 2067. PMID: 17459422.

Bennett et al (2001) SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase. Proc.Natl.Acad.Sci.U.S.A. 98 13681. PMID: 11717429.

Schnabl et al (2001) TAK1/JNK and p38 have opposite effects on rat hepatic stellate cells. Hepatology 34 953. PMID: 11679966.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SP 600125 include:

Rahman et al (2016) 18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis. Biochemical Pharmacology 117 97. PMID: 27520483.

Bulut et al (2015) Effects of jnk inhibitor on inflammation and fibrosis in the ovary tissue of a rat model of polycystic ovary syndrome. Exp Hematol Oncol 8 8774. PMID: 26464620.

Chen et al (2015) Black Rice Anthocyanins Suppress Metastasis of Breast Cancer Cells by Targeting RAS/RAF/MAPK Pathway. Int J Clin Exp Pathol 2015 414250. PMID: 26649302.

Edén et al (2015) Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated insulin secretion from human pancreatic islets. Diabetologia 58 2563. PMID: 26271343.

Karmakar et al (2015) Neutrophil IL-1β processing induced by pneumolysin is mediated by the NLRP3/ASC inflammasome and caspase-1 activation and is dependent on K+ efflux. Nat Commun 194 1763. PMID: 25609842.

Koerber et al (2015) Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma. Nat Commun 4 21. PMID: 26251761.

Liu et al (2015) Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment. Int J Mol Sci 5 79. PMID: 25999956.

Smith et al (2015) The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation. J Biol Chem 10 e0136546. PMID: 26414859.

Sommerfeld et al (2015) Free fatty acids shift insulin-induced hepatocyte proliferation towards CD95-dependent apoptosis. J Biomed Sci 290 4398. PMID: 25548285.

Yang et al (2015) Inhibition of G9a Histone Methyltransferase Converts Bone Marrow Mesenchymal Stem Cells to Cardiac Competent Progenitors. PLoS One 2015 270428. PMID: 26089912.

Yoshimura et al (2015) Inhibitory effect of statins on inflammation-related pathways in human abdominal aortic aneurysm tissue. Biomed Res Int 16 11213. PMID: 25993292.

Zhang et al (2015) Activation of transcription factor AP-1 in response to thermal injury in rat small intestine and IEC-6 cells. BMC Gastroenterol 15 83. PMID: 26162907.

Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. Steroids 5 4421. PMID: 25030704.

Bae et al (2014) Activation of pattern recognition receptors in brown adipocytes induces inflammation and suppresses uncoupling protein 1 expression and mitochondrial respiration. Am J Physiol Cell Physiol 306 C918. PMID: 24627558.

Basu et al (2014) Suppression of MAPK/JNK-MTORC1 signaling leads to premature loss of organelles and nuclei by autophagy during terminal differentiation of lens fiber cells. Autophagy 10 1193. PMID: 24813396.

El-Sayed et al (2014) P2Y2 nucleotide receptor activation enhances the aggregation and self-organization of dispersed salivary epithelial cells. J Cell Mol Med 307 C83. PMID: 24760984.

Gonsalves et al (2014) Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α. Am J Hematol 89 273. PMID: 24227191.

Huang et al (2014) Protective effect of Danggui (Radix Angelicae Sinensis) on angiotensin II-induced apoptosis in H9c2 cardiomyoblast cells. BMC Complement Altern Med 14 358. PMID: 25256260.

Kim et al (2014) AMP-activated protein kinase determines apoptotic sensitivity of cancer cells to ginsenoside-Rh2. J Ginseng Res 38 16. PMID: 24558305.

Kim et al (2014) Decrease of PKB/Akt Phosphorylation is Partially Mediated by SAPK/JNK Activation in Serum-free L6 Myoblasts Starved with Low Glucose. J Phys Ther Sci 26 1757. PMID: 25435694.

Martin et al (2014) miR-155 induced transcriptome changes in the MCF-7 breast cancer cell line leads to enhanced mitogen activated protein kinase signaling. Korean J Physiol Pharmacol 5 353. PMID: 25352952.

Yu et al (2014) Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation. PLoS One 9 e112989. PMID: 25398056.

Zhang et al (2014) Adiponectin ameliorates experimental periodontitis in diet-induced obesity mice. PLoS One 9 e97824. PMID: 24836538.

Enomoto et al (2013) Transcriptional regulation of an insulin-sensitizing adipokine adipolin/CTRP12 in adipocytes by Krüppel-like factor 15. Am J Physiol Lung Cell Mol Physiol 8 e83183. PMID: 24358263.

Stradner et al (2013) Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes. Genes Cancer 65 2113. PMID: 23666803.

Xiong et al (2013) Arginase-II induces vascular smooth muscle cell senescence and apoptosis through p66Shc and p53 independently of its l-arginine ureahydrolase activity: implications for atherosclerotic plaque vulnerability. J Am Heart Assoc 2 e000096. PMID: 23832324.

Akhmetshina et al (2012) Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis. Stem Cells Int 3 735. PMID: 22415826.

Chen et al (2012) Cyclic AMP increases COX-2 expression via mitogen-activated kinase in human myometrial cells. PLoS One 16 1447. PMID: 21854542.

Khuituan et al (2012) Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice. Am J Physiol Endocrinol Metab 302 E903. PMID: 22275752.

Lin et al (2012) Desipramine protects neuronal cell death and induces heme oxygenase-1 expression in Mes23.5 dopaminergic neurons. PLoS One 7 e50138. PMID: 23209658.

Meotti et al (2012) Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways. Br J Pharmacol 166 1127. PMID: 22220695.

Oberbach et al (2012) Free fatty acid palmitate impairs the vitality and function of cultured human bladder smooth muscle cells. Am J Physiol Cell Physiol 7 e41026. PMID: 22808290.

Schepetkin et al (2012) Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors. Mol Pharmacol 81 832. PMID: 22434859.

Hecker et al (2011) Reversible differentiation of myofibroblasts by MyoD. J Biol Chem 317 1914. PMID: 21440539.

Hsu et al (2011) JNK suppression is essential for 17β-Estradiol inhibits prostaglandin E2-Induced uPA and MMP-9 expressions and cell migration in human LoVo colon cancer cells. PLoS One 18 61. PMID: 21859479.

Kang et al (2011) MUC5AC expression through bidirectional communication of Notch and epidermal growth factor receptor pathways. J Immunol 187 222. PMID: 21622856.

Kim et al (2011) Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells. Nat Commun 15 211. PMID: 21994479.

Ye et al (2011) Dermatophagoides pteronyssinus 2 regulates nerve growth factor release to induce airway inflammation via a reactive oxygen species-dependent pathway. J Inflamm (Lond) 300 L216. PMID: 21097523.

Zhou and Too (2011) Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth. Arthritis Rheum 6 e21680. PMID: 21738764.

Ishida et al (2010) Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish. Dev Biol 340 468. PMID: 20144602.

Lee et al (2010) Prevention of premature senescence requires JNK regulation of Bcl-2 and reactive oxygen species. Oncogene 29 561. PMID: 19855432.

Zhou et al (2010) miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon production by human plasmacytoid dendritic cells. Blood 116 5885. PMID: 20852130.

Steubesand et al (2009) The expression of the beta-defensins hBD-2 and hBD-3 is differentially regulated by NF-kappaB and MAPK/AP-1 pathways in an in vitro model of Candida esophagitis. BMC Immunol 10 36. PMID: 19523197.

Yeligar et al (2009) Ethanol augments RANTES/CCL5 expression in rat liver sinusoidal endothelial cells and human endothelial cells via activation of NF-kappa B, HIF-1 alpha, and AP-1. J Immunol 183 5964. PMID: 19828633.

Yu et al (2009) c-Jun protects hypoxia-inducible factor-1alpha from degradation via its oxygen-dependent degradation domain in a nontranscriptional manner. Cancer Res 69 7704. PMID: 19738058.

Yun et al (2009) AMP kinase signaling determines whether c-Jun N-terminal kinase promotes survival or apoptosis during glucose deprivation. Carcinogenesis 30 529. PMID: 19037093.

Chen et al (2008) Ceramide induces p38 MAPK and JNK activation through a mechanism involving a thioredoxin-interacting protein-mediated pathway. Blood 111 4365. PMID: 18270325.

García-Escudero et al (2008) Glioma regression in vitro and in vivo by a suicide combined treatment. Exp Cell Res 6 407. PMID: 18337448.

Hoffmann et al (2008) Transcriptional regulation of EGR-1 by the interleukin-1-JNK-MKK7-c-Jun pathway. J Biol Chem 283 12120. PMID: 18281687.

Jung et al (2008) Reactive oxygen species stabilize hypoxia-inducible factor-1 alpha protein and stimulate transcriptional activity via AMP-activated protein kinase in DU145 human prostate cancer cells. Carcinogenesis 29 713. PMID: 18258605.

Moynihan et al (2008) MAP kinases mediate interleukin-13 effects on calcium signaling in human airway smooth muscle cells. Am J Physiol Lung Cell Mol Physiol 295 L171. PMID: 18441092.

Su et al (2008) 15-deoxy-Delta12,14-prostaglandin J2 up-regulates death receptor 5 gene expression in HCT116 cells: involvement of reactive oxygen species and C/EBP homologous transcription factor gene transcription. Mol Cancer Ther 7 3429. PMID: 18852146.

Wolter et al (2008) c-Jun controls histone modifications, NF-kappaB recruitment, and RNA polymerase II function to activate the ccl2 gene. Mol Cell Biol 28 4407. PMID: 18443042.

Su et al (2007) 5-Aminoimidazole-4-carboxamide riboside sensitizes TRAIL- and TNF{alpha}-induced cytotoxicity in colon cancer cells through AMP-activated protein kinase signaling. Mol Cancer Ther 6 1562. PMID: 17513605.

Zhou et al (2007) Delayed and persistent ERK1/2 activation is required for 4-hydroxytamoxifen-induced cell death. Mol Cancer Res 72 765. PMID: 17714751.

Guillemot and Citi (2006) Cingulin regulates claudin-2 expression and cell proliferation through the small GTPase RhoA. Mol Biol Cell 17 3569. PMID: 16723500.

Kauppinen et al (2006) Direct phosphorylation and regulation of poly(ADP-ribose) polymerase-1 by extracellular signal-regulated kinases 1/2. Proc Natl Acad Sci U S A 103 7136. PMID: 16627622.

Kim et al (2006) Transforming growth factor-beta1 regulates macrophage migration via RhoA. Blood 108 1821. PMID: 16705092.

Olsson and Sundler (2006) Different roles for non-receptor tyrosine kinases in arachidonate release induced by zymosan and Staphylococcus aureus in macrophages. J Immunol 3 8. PMID: 16674821.

Shacka et al (2006) Two distinct signaling pathways regulate peroxynitrite-induced apoptosis in PC12 cells. Cardiorenal Med 13 1506. PMID: 16410804.

Sunters et al (2006) Paclitaxel-induced nuclear translocation of FOXO3a in breast cancer cells is mediated by c-Jun NH2-terminal kinase and Akt. Cancer Res 66 212. PMID: 16397234.

Wang et al (2006) Paclitaxel (Taxol) upregulates expression of functional interleukin-6 in human ovarian cancer cells through multiple signaling pathways. Oncogene 25 4857. PMID: 16547493.

Hoffmann et al (2005) MEK1-dependent delayed expression of Fos-related antigen-1 counteracts c-Fos and p65 NF-kappaB-mediated interleukin-8 transcription in response to cytokines or growth factors. J Biol Chem 280 9706. PMID: 15615716.

Lee et al (2005) Estrogen receptor alpha pathway is involved in the regulation of Calbindin-D9k in the uterus of immature rats. Toxicol Sci 84 270. PMID: 15635152.

Ma et al (2005) Oxygen-sensitive {δ}-opioid receptor-regulated survival and death signals: novel insights into neuronal preconditioning and protection. PLoS One 280 16208. PMID: 15687501.

Yun et al (2005) Glucose deprivation increases mRNA stability of vascular endothelial growth factor through activation of AMP-activated protein kinase in DU145 prostate carcinoma. Blood 280 9963. PMID: 15640157.

Campàs et al (2003) Acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes. Cell Death Differ 101 3674. PMID: 12522004.

Holzberg et al (2003) Disruption of the c-JUN-JNK complex by a cell-permeable peptide containing the c-JUN delta domain induces apoptosis and affects a distinct set of interleukin-1-induced inflammatory genes. J Biol Chem 278 40213. PMID: 12832416.

Stähle et al (2003) Mechanisms in LPA-induced tumor cell migration: critical role of phosphorylated ERK. J Cell Sci 116 3835. PMID: 12902401.

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