货品编号： Mce.HY-10295

品牌： Mce

品名： SB 20219010 mg

规格： 10 mg

生物活性

SB 202190 is a highly selective, potent and cell-permeable inhibitor of p38 MAP kinase with IC50 values of 50 nM and

100 nM for p38α and p38β respectively; also showed slightly weaker activity for BRD4 (Kd=3.4 uM).

IC50 value: 50 nM (p38α); 100 nM (p38β) [1]

in vitro: SB202190 binds within the ATP pocket of the active kinase (Kd = 38 nM, as measured in recombinant human p38),

and selectively inhibits the p38α and β isoforms (IC50 = 50 and 100 nM at SAPK2a/p38 and SAPK2b/p38β2 respectively) [1].

SB202190 by itself was sufficient to induce cell death, with typical apoptotic features such as nucleus condensation and

intranucleosomal DNA fragmentation. SB202190 stimulated the activity of CPP32-like caspases, and its apoptotic effect was

completely blocked by the protease inhibitor benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone and expression of bcl-2.

In addition, SB202190 was able to potentiate apoptosis induced by Fas(APO-1) ligation or UV irradiation. Expression of p38beta

attenuated the apoptotic effect of SB202190 and the cell death induced by Fas ligation and UV irradiation [2]. The p38 inhibitor

SB-202190 and the PI3K inhibitor PP-242 showed slightly weaker activity (Kd values: 3.4 ± 0.13 μM and 1.7 ± 0.076 μM, respectively) [5].

in vivo: Inhibiting p38 by administration of SB 202190 inhibits PV IgG-induced blister formation in the passive transfer mouse model [3].

In the endotoxin model of sepsis, SB 202190 treatment produces a statistically significant survival benefit compared with control [4].