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Cat. No. Name Size Price Add Cart
KI0580SP60012510 mg$100
SP60012525 mg$170
SP600125250 mg$1300

Chemical Characteristic

Product NameSP600125
CAS No.129-56-6
Molecular Weight 220.23
FormulaC14H8N2O
Chemical NameAnthra[1,9-cd]pyrazol-6(2H)-one
Smilesn1[nH]c2c3c1c1c(c(=O)c3ccc2)cccc1
Chemical Structure

Biological activities

SP600125 is a selective inhibitor of Jun N-terminal kinase (JNK). SP600125 inhibits JNK1, JNK2 and JNK3 kinases with IC50 of 40, 40 and 90 nM, respectively. SP600125 also selectively inhibits p56Lck, MKK4, MKK3, MKK6, PKB and PKCa kinases with IC50 of 4.3, 0.4, 1.5, 1.0, 1.0 and 1.5 μM, respectively. In cells stimulated with phorbol 12-myristate 13-acetate (PMA) and phytohemagglutinin, SP600125 dose-dependently blocks both IL-2 and IFN-γ expression with IC50 of 6 and 7 μM, respectively. The levels of COX-2 and TNF-a mRNA are dose-dependently inhibited by SP600125 with IC50 of 5 and 10 μM, respectively. In cells, SP600125 dose dependently prevents the activation and differentiation of primary human CD4 cell cultures.[1] In OVCAR-3 cells, SP600125 inhibits the PMA-dependent secretion of MMP-9 in a time-dependent manner. SP600125 represses the activity of a PMA-stimulated MMP-9 promoter-driven luciferase reporter. [2] SP600125 can inhibit the activation of the JNK-c-Jun-FasL pathway and protect renal tubular epithelial cells against ischemia/reperfusion-induced apoptosis. SP600125 attenuates the increased expression of FasL induced by ischemia/reperfusion at 3 hours. [3] SP600125 significantly induces CYP1A1 and CYP1A2 mRNAs in primary human hepatocytes and CYP1A1 mRNA in human hepatoma cells HepG2. SP600125 dose-dependently inhibits CYP1A1 and CYP1A2 genes induction by a prototype AhR ligand 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) in human hepatocytes. SP600125 transactivates the pDRE-luc and p1A1-luc reporter plasmids with EC50 of 5 nM and 1.89 μM, respectively. TCDD-dependent transactivation of the reporter plasmids is inhibited by SP600125 with IC50 of 1.54 and 2.63 μM, respectively. [4] In animal studies, SP600125 blocks (bacterial) lipopolysaccharide- induced expression of tumor necrosis factor-a and inhibits anti-CD3-induced apoptosis of CD4+ CD8+ thymocytes. [1] SP600125 significantly reduces eosinophil and lymphocyte numbers in bronchoalveolar lavage fluid, suppresses eosinophilic inflammation within the bronchial submucosa, inhibits goblet cell hyperplasia, and increases airway smooth muscle cell number in allergen-exposed mice. SP600125 also inhibits allergen-induced increase in bronchial responsiveness. [5]

Protocols

SP600125 is dissolved in DMSO. [1]

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.
[2] Shin M, et al. An inhibitor of c-jun aminoterminal kinase (SP600125) represses c-Jun activation, DNA-binding and PMA-inducible 92-kDa type IV collagenase expression. Biochim Biophys Acta. 2002, 1589(3): 311-316.
[3] Wang Y, et al. SP600125, a selective JNK inhibitor, protects ischemic renal injury via suppressing the extrinsic pathways of apoptosis. Life Sci. 2007, 80(22): 2067-2075.
[4] Dvorak Z, et al. JNK inhibitor SP600125 is a partial agonist of human aryl hydrocarbon receptor and induces CYP1A1 and CYP1A2 genes in primary human hepatocytes. Biochem Pharmacol. 2008, 75(2): 580-588.
[5] Nath P, et al. Potential role of c-Jun NH2-terminal kinase in allergic airway inflammation and remodelling: effects of SP600125. Eur J Pharmacol. 2005, 506(3): 273-283.

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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