SB203580

SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.

Synonyms:

PB 203580;

4-(4-(4-Fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine;

4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(pyridin-4-yl)-1H-imidazole;

RWJ 64809;

Pyridine,4-(5-(4-fluorophenyl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-4-yl);

Properties:

Appearance & Physical State:  White solid

Density: 1.42 g/cm3

Boiling Point: 615.6ºC at 760 mmHg

Melting Point: 249 - 250ºC

Flash Point: 326.1ºC

Refractive Index: 1.714

Vapor Pressure: 2E-14mmHg at 25°C

p38 MAPK Inhibitors Related Products:

Doramapimod; SB-202190; VX-702; PH-797804; Neflamapimod; TAK-715; R1487 HCl; SB239063; Losmapimod; Ralimetinib dimesylate

[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.