SB 203580 (152121-47-6) is a potent and selective inhibitor of p38 MAP kinase, IC50=50 and 500 nM for p38 and p38β2 respectively.1 No other kinases (in a panel of 30) were significantly inhibited including p38γ and δ at 10 μM.2 A potent inhibitor of inflammatory cytokine production (IC50=15-25 mg/kg in mice and rats) in animal models of arthritis, bone resorption, endotoxin shock and immune function.3 SB 203580(152121-47-6)是p38 MAP激酶的选择性抑制剂,对p38和p38β2的IC50分别为50和500 nM 其他激酶(30个)均未被显著抑制,包括p38γ和δ在10 μM.2 在关节炎、骨吸收、内毒素休克和免疫功能的动物模型中,抑制炎症细胞因子产生(小鼠和大鼠IC50=15-25 mg/kg)
References/Citations:
1) Cuenda et al. (1995), SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin-1; FEBS Lett., 364 229 2) Davies et al. (2000), Specificity and mechanism of action of some commonly used protein kinase inhibitors; Biochem. J., 351 95 3) Badger et al. (1996), Pharmacological profile of SB 203580, a selective inhibitor of cytokine suppressive binding protein/p38 kinase, in animal models of arthritis, bone resorption, endotoxin shock and immune function; Pharmacol. Exp. Ther. 279 1453
CAS:
152121-47-6
Catalog Number:
10-2173
Activity:
p38 MAP kinase inhibitor
Chemical Name:
4-(4-Fluorophenyl)-2-(4-methylsulfinylphenyl)-5-(4-pyridyl)imidazole
Molecular Weight:
377.44
Molecular Formula:
C21H16N3OSF
Solubility:
Soluble in DMSO (up to 100 mg/ml) or in Ethanol (up to 10 mg/ml with warming).
Physical Properties:
Off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT
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