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.
|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.
|Related p38 MAPK Products|
TA-02 is a p38 MAPK inhibitor with IC50 of 20 nM. IC50 value: 20 nM. TA-02 is a novel compound with similar cardiogenic properties as SB203580 and SB202190. TA-02 especially inhibits TGFBR-2.
Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
Losmapimod (GW856553) is a selective, potent, and orally active p38 MAPK inhibitor with pKi of 8.1 and 7.6 for p38α and p38β, respectively.
VX-745 is a potent and selective inhibitor of p38α with IC50 of 10 nM, 22-fold greater selectivity versus p38β and no inhibition to p38γ.
TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
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