SB 202190

Selective, potent and cell permeable inhibitor of p38 MAP kinase.

Prod. No. S 7067

The p38 subfamily of MAP kinases (p38 MAPK) consists of p38a, p38b, p38g, and p38d and regulates gene expression in response to various extracellular stimuli including growth factors, hormones, ligands for G protein coupled receptors, inflammatory cytokines (IL-1, IL-8, TNFa) and stresses (heat, osmotic shock). Because of its critical role in inflammation and stress response, p38 MAPK is of great interest in both basic and therapeutic research.^1-3

Sigma-RBI is please to introduce SB 202190, a potent, selective and cell permeable p38 MAPK inhibitor:

• Binds to the ATP binding site on active p38 MAPK with a K_d value of 38 nM for recombinant p38 and 30-50 nM for the native protein.³
• Selectively inhibits p38a and b isoforms (IC₅₀ = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38b2 respectively).⁴
• Selectively binds p38 and has no effect on JNK, p42/44^MAPK or other multiple related protein kinases at concentrations up to 100 µM.⁴
• Induces apoptosis in Jurkat and HeLa cells in vitro with typical apoptotic features including nucleus condensation and DNA fragmentation.⁵
• At 1 µmol/l, inhibits p38-MAPK in human mesanglial cells and reduces hexosamine-induced TGFb1 expression at normal (7 mmol/l), as well as high (25 mmol/l) glucose levels, implicating the p38 pathway in the pathophysiology of diabetic glomerulopathy.⁶

Physical Description: Solubility: Molecular Formula: Formula Weight: Sizes:

Off-white solid Soluble in DMSO at 30 mg/ml C20H14N3OF 331.35 5 mg, 25 mg

Sold for research purposes under agreement from GlaxoSmithKline

References

1. Johnson, G.L., et al., Science, 298, 1911-1912 (2002).
2. Wilson, K.P., et al., Chem. Biol., 4, 423-431 (1997).
3. Frantz, B., et al., Biochemistry, 37, 13846-13853 (1998).
4. Davies, S.P., et al., Biochem. J., 351, 95-105 (2000).
5. Nemoto,S., et al., J. Biol. Chem, 273, 16415-16420 (1998).
6. Burt, D.J., et al., Diabetologia, 46, 531-537 (2003).

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