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

M.Wt:
220.23
Formula:
C14H8N2O
Solubility:
Soluble to 5 mM in ethanol with gentle warming and to 100 mM in DMSO
Purity:
>98 %
Storage:
Desiccate at -20°C
CAS No:
129-56-6

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:

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.

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.

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.

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.

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.

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.

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.

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

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

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.

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.

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.

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.

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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Keywords: SP 600125, supplier, selective, JNK, inhibitor, MAPK, Signaling, Signalling, c-Jun, N-Terminal, Kinase, SAPKs, Stress-Activated, Protein, Mitogen-Activated, SP600125, Tocris Bioscience, JNK/c-Jun Inhibitor products

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