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Datasheet of SB202190
Description: 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). 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). 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. 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). in vivo: Inhibiting p38 by administration of SB 202190 inhibits PV IgG-induced blister formation in the passive transfer mouse model. In the endotoxin model of sepsis, SB 202190 treatment produces a statistically significant survival benefit compared with control.
Chemical Information Catalog
DC2097
Purity of current batch:
>98%
Molecular Weight (MW)
331.34
Molecular Formula
C20H14N3OF
CAS No.
152121-30-7
Solubility (25°C)
DMSO