Catalog Number: 1496
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.
Background References
  1. SP600125, an anthrapyrazolone inhibitor of Jun N-terminal kinase.
    Bennett et al.
    Proc.Natl.Acad.Sci.U.S.A., 2001;98:13681
  2. TAK1/JNK and p38 have opposite effects on rat hepatic stellate cells.
    Schnabl et al.
    Hepatology, 2001;34:953
  3. SP600125, a selective JNK inhibitor, protects ischemic renal injury via suppressing the extrinsic pathways of apoptosis.
    Wang et al.
    Life Sci., 2007;80:2067
  4. Activation of JNKs is essential for BMP9-induced osteogenic differentiation of mesenchymal stem cells.
    Zhao et al.
    BMB Rep., 2013;46:422
  5. Derivation of novel human ground state naive pluripotent stem cells.
    Gafni et al.
    Nature, 2013;504:282
Citations:

The citations listed below are publications that use Tocris products. Selected citations for SP 600125 include:

71 Citations: Showing 1 - 10
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  1. TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells.
    Authors: Wu
    Arch Biochem Biophys 2017;622:26
  2. Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation.
    Authors: Han
    Brain Res 2017;1663:132
  3. 18α-glycyrrhetinic acid lethality for neuroblastoma cells via de-regulating the Beclin-1/Bcl-2 complex and inducing apoptosis.
    Authors: Rahman Et al.
    Biochemical Pharmacology 2016;117:97
  4. Effects of jnk inhibitor on inflammation and fibrosis in the ovary tissue of a rat model of polycystic ovary syndrome.
    Authors: Bulut Et al.
    Exp Hematol Oncol 2015;8:8774
  5. Hyperphosphate-Induced Myocardial Hypertrophy through the GATA-4/NFAT-3 Signaling Pathway Is Attenuated by ERK Inhibitor Treatment.
    Authors: Liu Et al.
    Int J Mol Sci 2015;5:79
  6. Tissue factor/factor VIIa signalling promotes cytokine-induced beta cell death and impairs glucose-stimulated insulin secretion from human pancreatic islets.
    Authors: Edén Et al.
    Diabetologia 2015;58:2563
  7. Analysis of the anti-proliferative and the pro-apoptotic efficacy of Syk inhibition in multiple myeloma.
    Authors: Koerber Et al.
    Nat Commun 2015;4:21
  8. Free fatty acids shift insulin-induced hepatocyte proliferation towards CD95-dependent apoptosis.
    Authors: Sommerfeld Et al.
    J Biomed Sci 2015;290:4398
  9. Black Rice Anthocyanins Suppress Metastasis of Breast Cancer Cells by Targeting RAS/RAF/MAPK Pathway.
    Authors: Chen Et al.
    Int J Clin Exp Pathol 2015;2015:414250
  10. Inhibition of G9a Histone Methyltransferase Converts Bone Marrow Mesenchymal Stem Cells to Cardiac Competent Progenitors.
    Authors: Yang Et al.
    PLoS One 2015;2015:270428
  11. Neutrophil IL-1β processing induced by pneumolysin is mediated by the NLRP3/ASC inflammasome and caspase-1 activation and is dependent on K+ efflux.
    Authors: Karmakar Et al.
    Nat Commun 2015;194:1763
  12. Inhibitory effect of statins on inflammation-related pathways in human abdominal aortic aneurysm tissue.
    Authors: Yoshimura Et al.
    Biomed Res Int 2015;16:11213
  13. Activation of transcription factor AP-1 in response to thermal injury in rat small intestine and IEC-6 cells.
    Authors: Zhang Et al.
    BMC Gastroenterol 2015;15:83
  14. The Effects of the Endocannabinoids Anandamide and 2-Arachidonoylglycerol on Human Osteoblast Proliferation and Differentiation.
    Authors: Smith Et al.
    J Biol Chem 2015;10:e0136546
  15. Adiponectin ameliorates experimental periodontitis in diet-induced obesity mice.
    Authors: Zhang Et al.
    PLoS One 2014;9:e97824
  16. Differential effects of the Toll-like receptor 2 agonists, PGN and Pam3CSK4 on anti-IgE induced human mast cell activation.
    Authors: Yu Et al.
    PLoS One 2014;9:e112989
  17. Angiogenic growth factors augment K-Cl cotransporter expression in erythroid cells via hypoxia-inducible factor-1α.
    Authors: Gonsalves Et al.
    Am J Hematol 2014;89:273
  18. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    Steroids 2014;5:4421
  19. miR-155 induced transcriptome changes in the MCF-7 breast cancer cell line leads to enhanced mitogen activated protein kinase signaling.
    Authors: Martin Et al.
    Korean J Physiol Pharmacol 2014;5:353
  20. AMP-activated protein kinase determines apoptotic sensitivity of cancer cells to ginsenoside-Rh2.
    Authors: Kim Et al.
    J Ginseng Res 2014;38:16
  21. P2Y2 nucleotide receptor activation enhances the aggregation and self-organization of dispersed salivary epithelial cells.
    Authors: El-Sayed Et al.
    J Cell Mol Med 2014;307:C83
  22. Activation of pattern recognition receptors in brown adipocytes induces inflammation and suppresses uncoupling protein 1 expression and mitochondrial respiration.
    Authors: Bae Et al.
    Am J Physiol Cell Physiol 2014;306:C918
  23. Decrease of PKB/Akt Phosphorylation is Partially Mediated by SAPK/JNK Activation in Serum-free L6 Myoblasts Starved with Low Glucose.
    Authors: Kim Et al.
    J Phys Ther Sci 2014;26:1757
  24. Protective effect of Danggui (Radix Angelicae Sinensis) on angiotensin II-induced apoptosis in H9c2 cardiomyoblast cells.
    Authors: Huang Et al.
    BMC Complement Altern Med 2014;14:358
  25. Suppression of MAPK/JNK-MTORC1 signaling leads to premature loss of organelles and nuclei by autophagy during terminal differentiation of lens fiber cells.
    Authors: Basu Et al.
    Autophagy 2014;10:1193
  26. Transcriptional regulation of an insulin-sensitizing adipokine adipolin/CTRP12 in adipocytes by Krüppel-like factor 15.
    Authors: Enomoto Et al.
    Am J Physiol Lung Cell Mol Physiol 2013;8:e83183
  27. Sphingosine 1-phosphate counteracts the effects of interleukin-1β in human chondrocytes.
    Authors: Stradner Et al.
    Genes Cancer 2013;65:2113
  28. 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.
    Authors: Xiong Et al.
    J Am Heart Assoc 2013;2:e000096
  29. Identification and characterization of a novel class of c-Jun N-terminal kinase inhibitors.
    Authors: Schepetkin Et al.
    Mol Pharmacol 2012;81:832
  30. Desipramine protects neuronal cell death and induces heme oxygenase-1 expression in Mes23.5 dopaminergic neurons.
    Authors: Lin Et al.
    PLoS One 2012;7:e50138
  31. Free fatty acid palmitate impairs the vitality and function of cultured human bladder smooth muscle cells.
    Authors: Oberbach Et al.
    Am J Physiol Cell Physiol 2012;7:e41026
  32. Activation of canonical Wnt signalling is required for TGF-β-mediated fibrosis.
    Authors: Akhmetshina Et al.
    Stem Cells Int 2012;3:735
  33. Fibroblast growth factor-23 abolishes 1,25-dihydroxyvitamin D3-enhanced duodenal calcium transport in male mice.
    Authors: Khuituan Et al.
    Am J Physiol Endocrinol Metab 2012;302:E903
  34. Cyclic AMP increases COX-2 expression via mitogen-activated kinase in human myometrial cells.
    Authors: Chen Et al.
    PLoS One 2012;16:1447
  35. Inflammatory muscle pain is dependent on the activation of kinin B1 and B2 receptors and intracellular kinase pathways.
    Authors: Meotti Et al.
    Br J Pharmacol 2012;166:1127
  36. Mitochondrial localized STAT3 is involved in NGF induced neurite outgrowth.
    Authors: Zhou and Too
    Arthritis Rheum 2011;6:e21680
  37. Reversible differentiation of myofibroblasts by MyoD.
    Authors: Hecker Et al.
    J Biol Chem 2011;317:1914
  38. Dermatophagoides pteronyssinus 2 regulates nerve growth factor release to induce airway inflammation via a reactive oxygen species-dependent pathway.
    Authors: Ye Et al.
    J Inflamm (Lond) 2011;300:L216
  39. 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.
    Authors: Hsu Et al.
    PLoS One 2011;18:61
  40. MUC5AC expression through bidirectional communication of Notch and epidermal growth factor receptor pathways.
    Authors: Kang Et al.
    J Immunol 2011;187:222
  41. Thrombin-induced Migration and Matrix Metalloproteinase-9 Expression Are Regulated by MAPK and PI3K Pathways in C6 Glioma Cells.
    Authors: Kim Et al.
    Nat Commun 2011;15:211
  42. Phosphorylation of Junb family proteins by the Jun N-terminal kinase supports tissue regeneration in zebrafish.
    Authors: Ishida Et al.
    Dev Biol 2010;340:468
  43. Prevention of premature senescence requires JNK regulation of Bcl-2 and reactive oxygen species.
    Authors: Lee Et al.
    Oncogene 2010;29:561
  44. miR-155 and its star-form partner miR-155* cooperatively regulate type I interferon production by human plasmacytoid dendritic cells.
    Authors: Zhou Et al.
    Blood 2010;116:5885
  45. c-Jun protects hypoxia-inducible factor-1alpha from degradation via its oxygen-dependent degradation domain in a nontranscriptional manner.
    Authors: Yu Et al.
    Cancer Res 2009;69:7704
  46. AMP kinase signaling determines whether c-Jun N-terminal kinase promotes survival or apoptosis during glucose deprivation.
    Authors: Yun Et al.
    Carcinogenesis 2009;30:529
  47. 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.
    Authors: Yeligar Et al.
    J Immunol 2009;183:5964
  48. 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.
    Authors: Steubesand Et al.
    BMC Immunol 2009;10:36
  49. 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.
    Authors: Su Et al.
    Mol Cancer Ther 2008;7:3429
  50. Glioma regression in vitro and in vivo by a suicide combined treatment.
    Authors: García-Escudero Et al.
    Exp Cell Res 2008;6:407
  51. 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.
    Authors: Jung Et al.
    Carcinogenesis 2008;29:713
  52. MAP kinases mediate interleukin-13 effects on calcium signaling in human airway smooth muscle cells.
    Authors: Moynihan Et al.
    Am J Physiol Lung Cell Mol Physiol 2008;295:L171
  53. c-Jun controls histone modifications, NF-kappaB recruitment, and RNA polymerase II function to activate the ccl2 gene.
    Authors: Wolter Et al.
    Mol Cell Biol 2008;28:4407
  54. Transcriptional regulation of EGR-1 by the interleukin-1-JNK-MKK7-c-Jun pathway.
    Authors: Hoffmann Et al.
    J Biol Chem 2008;283:12120
  55. Ceramide induces p38 MAPK and JNK activation through a mechanism involving a thioredoxin-interacting protein-mediated pathway.
    Authors: Chen Et al.
    Blood 2008;111:4365
  56. Delayed and persistent ERK1/2 activation is required for 4-hydroxytamoxifen-induced cell death.
    Authors: Zhou Et al.
    Mol Cancer Res 2007;72:765
  57. 5-Aminoimidazole-4-carboxamide riboside sensitizes TRAIL- and TNF{alpha}-induced cytotoxicity in colon cancer cells through AMP-activated protein kinase signaling.
    Authors: Su Et al.
    Mol Cancer Ther 2007;6:1562
  58. Paclitaxel-induced nuclear translocation of FOXO3a in breast cancer cells is mediated by c-Jun NH2-terminal kinase and Akt.
    Authors: Sunters Et al.
    Cancer Res 2006;66:212
  59. Different roles for non-receptor tyrosine kinases in arachidonate release induced by zymosan and Staphylococcus aureus in macrophages.
    Authors: Olsson and Sundler
    J Immunol 2006;3:8
  60. Paclitaxel (Taxol) upregulates expression of functional interleukin-6 in human ovarian cancer cells through multiple signaling pathways.
    Authors: Wang Et al.
    Oncogene 2006;25:4857
  61. Cingulin regulates claudin-2 expression and cell proliferation through the small GTPase RhoA.
    Authors: Guillemot and Citi
    Mol Biol Cell 2006;17:3569
  62. Two distinct signaling pathways regulate peroxynitrite-induced apoptosis in PC12 cells.
    Authors: Shacka Et al.
    Cardiorenal Med 2006;13:1506
  63. Transforming growth factor-beta1 regulates macrophage migration via RhoA.
    Authors: Kim Et al.
    Blood 2006;108:1821
  64. Direct phosphorylation and regulation of poly(ADP-ribose) polymerase-1 by extracellular signal-regulated kinases 1/2.
    Authors: Kauppinen Et al.
    Proc Natl Acad Sci U S A 2006;103:7136
  65. Estrogen receptor alpha pathway is involved in the regulation of Calbindin-D9k in the uterus of immature rats.
    Authors: Lee Et al.
    Toxicol Sci 2005;84:270
  66. Glucose deprivation increases mRNA stability of vascular endothelial growth factor through activation of AMP-activated protein kinase in DU145 prostate carcinoma.
    Authors: Yun Et al.
    Blood 2005;280:9963
  67. 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.
    Authors: Hoffmann Et al.
    J Biol Chem 2005;280:9706
  68. Oxygen-sensitive {δ}-opioid receptor-regulated survival and death signals: novel insights into neuronal preconditioning and protection.
    Authors: Ma Et al.
    PLoS One 2005;280:16208
  69. 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.
    Authors: Holzberg Et al.
    J Biol Chem 2003;278:40213
  70. Mechanisms in LPA-induced tumor cell migration: critical role of phosphorylated ERK.
    Authors: Stähle Et al.
    J Cell Sci 2003;116:3835
  71. Acadesine activates AMPK and induces apoptosis in B-cell chronic lymphocytic leukemia cells but not in T lymphocytes.
    Authors: Campàs Et al.
    Cell Death Differ 2003;101:3674
Expand to show all 71 Citations

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