SB 203580 hydrochloride

• CAT Number: I005227
• CAS Number: 869185-85-3
• Molecular Formula: C21H16FN3OS • HCl
• Molecular Weight: 413.9
• Purity: ≥95%
• Target: p38
• Solubility: ethanol:30 mg/ml;DMSO:30 mg/ml;DMF:30 mg/ml
• Storage: Store at -20C
• IC50: 0.3 -0.5 mM
• IUPAC Name: 4-[4-(4-fluorophenyl)-2-(4-methylsulfinylphenyl)-1H-imidazol-5-yl]pyridine;hydrochloride
• InChI: InChI=1S/C21H16FN3OS.ClH/c1-27(26)18-8-4-16(5-9-18)21-24-19(14-2-6-17(22)7-3-14)20(25-21)15-10-12-23-13-11-15;/h2-13H,1H3,(H,24,25);1H
• InChIKey: WOSGGXINSLMASH-UHFFFAOYSA-N
• SMILES: CS(=O)C1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC=C(C=C4)F.Cl

SB203580 hydrochloride (Cat No.:I005227) is a selective, ATP-competitive p38MAPK inhibitor with IC50 of 50nM and 500nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB203580 hydrochloride inhibits LCK, GSK3β and PKBα with IC50 100-500 times higher than SAPK2a/p38. SB203580 hydrochloride is an autophagy and mitosis activator.

Reference

[1]. Lali FV, et al. The pyridinyl imidazole inhibitor SB203580 blocks phosphoinositide-dependent protein kinase activity, protein kinase B phosphorylation, and retinoblastoma hyperphosphorylation in interleukin-2-stimulated T cells independently of p38 mitogen-activated protein kinase. J Biol Chem. 2000 Mar 10;275(10):7395-402.
[2]. Birkenkamp KU, et al. The p38 MAP kinase inhibitor SB203580 enhances nuclear factor-kappa B transcriptional activity by a non-specific effect upon the ERK pathway. Br J Pharmacol. 2000 Sep;131(1):99-107.
[3]. Zhang H, et al. Induction of autophagy in hepatocellular carcinoma cells by SB203580 requires activation of AMPK and DAPK but not p38 MAPK. Apoptosis. 2012 Apr;17(4):325-34.
[4]. Barancik M, et al. Inhibition of the cardiac p38-MAPK pathway by SB203580 delays ischemic cell death. J Cardiovasc Pharmacol. 2000 Mar;35(3):474-83.
[5]. Jin N, et al. The selective p38 mitogen-activated protein kinase inhibitor, SB203580, improves renal disease in MRL/lpr mouse model of systemic lupus. Int Immunopharmacol. 2011 Sep;11(9):1319-26.