SB 202190 is a potent p38 MAPK inhibitor. SB 202190 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). SB 202190 by itself was sufficient to induce cell death, with typical apoptotic features such as nucleus condensation and intranucleosomal DNA fragmentation. SB 202190 stimulated the activity of CPP32-like caspases, and its apoptotic effect was completely blocked by the expression of bcl-2. When tested at 10 μM, SB 202190 has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs). Recently, SB 202190 has been used to elucidate the roles of p38 MAP kinases in inflammatory cytokine expression, nicotine-induced receptor expression, and HIV-mediated depressive disorder.
|Source||Br J Pharmacol (2006). Figure 1. SB 202190|
|Cell Lines||HEK293 cells|
|Incubation Time||18 h|
|Results||The MAPK inhibitor, SB-202190, also antagonized human P2X7 receptor-mediated responses but was generally less potent than SB-203580 with pIC50 values varying from 6.2 to 4.8, depending on BzATP concentration.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 50 mg/mL|
Targeting the p38 MAPK pathway inhibits irinotecan resistance in colon adenocarcinoma.
Paillas S, et al. Cancer Res. 2011 Feb 1;71(3):1041-9. PMID: 21159664.
Activation of c-Jun N-terminal kinase (JNK) by widely used specific p38 MAPK inhibitors SB202190 and SB203580: a MLK-3-MKK7-dependent mechanism.
Muniyappa H, et al. Cell Signal. 2008 Apr;20(4):675-83. PMID: 18222647.
Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase.
Nemoto S, et al. J Biol Chem. 1998 Jun 26;273(26):16415-20. PMID: 9632706.
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SB 239063 is a potent and selective p38 MAPK inhibitor (IC50 = 44 nM for p38α). SB 239063 displays > 220-fold selectivity over ERK, JNK1 and other kinases; ~ 3-fold more selective than SB 203580.
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