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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
Storage
Store at -20째C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20째C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.