SP 600125

Pricing Availability Delivery Time Qty
Cat.No. 1496 - SP 600125 | C14H8N2O | CAS No. 129-56-6
Description: Selective JNK inhibitor
Chemical Name: Anthra[1-9-cd]pyrazol-6(2H)-one
Purity: ≥98% (HPLC)
Datasheet
Citations (71)
Literature
Pathways

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™.

Compound Libraries

SP 600125 is also offered as part of the Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 220.23
Formula C14H8N2O
Storage Desiccate at -20°C
Purity ≥98% (HPLC)
CAS Number 129-56-6
PubChem ID 8515
InChI Key ACPOUJIDANTYHO-UHFFFAOYSA-N
Smiles O=C1C2=C3C(NN=C3C3=CC=CC=C13)=CC=C2

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 22.02 100
ethanol 1.1 5mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 220.23. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.54 mL 22.7 mL 45.41 mL
5 mM 0.91 mL 4.54 mL 9.08 mL
10 mM 0.45 mL 2.27 mL 4.54 mL
50 mM 0.09 mL 0.45 mL 0.91 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References

References are publications that support the products' biological activity.

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

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

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

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


If you know of a relevant reference for SP 600125, please let us know.

View Related Products by Product Action

View all JNK/c-Jun Inhibitors

Keywords: selective JNK inhibitors inhibits MAPK Signaling Signalling c-Jun N-Terminal Kinase SAPKs Stress-Activated Protein Mitogen-Activated SP600125 JNK/c-jun

71 Citations for SP 600125

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Wu (2017) TRIB3 downregulation enhances doxorubicin-induced cytotoxicity in gastric cancer cells. Arch Biochem Biophys 622 26 PMID: 28442401

Han (2017) Cannabinoid receptor 1 contributes to sprouted innervation in endometrial ectopic growth through mitogen-activated protein kinase activation. Brain Res 1663 132 PMID: 28322749

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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


Do you know of a great paper that uses SP 600125 from Tocris? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Immunology

Immunology Product Listing

A collection of over 190 products for immunology research, the guide includes research tools for the study of:

  • Chemokine and Cytokine Signaling
  • Chemotaxis
  • Complement System
  • Immune Cell Signaling
  • Inflammation
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
MAPK Signaling

MAPK Signaling Scientific Review

MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.

Pathways for SP 600125

MAPK

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.

Protocols

TODO: Add Protocols