SB202190 (FHPI) |
| Catalog No.GC13968 |
SB202190 (FHPI) is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively.
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Cas No.: 152121-30-7
Sample solution is provided at 25 µL, 10mM.
SB 202190 is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 has anti-cancer activity and rescued memory deficits[1,2]. SB202190 inhibits apoptosis of endothelial cells by inducing autophagy and heme oxidase 1 [3].
SB 202190(50 µM;24 hours) significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner. SB202190 by itself is sufficient to induce cell death in Jurkat and HeLa cells through activation of CPP32-like caspases, which can be blocked by expression of bcl-2. SB202190-induced apoptosis is attenuated by p38β but augmented by p38α[4]. SB 202190 treatment(5/10 µM SB202190;4h) induces phosphorylation of JNK in a dose- and time- dependent manner in A549 cells, induces phosphorylation of ATF-2 transcription factor, and increases AP-1 DNA binding[5]. SB 202190(5µM;1h) strongly inhibits UVB induced COX-2 protein expression in HaCaT cells, and markedly inhibits UVB induced cox-2 mRNA[6].
SB 202190(12.5 µg; i.d.) attenuated blister formation induced by human poliomyelitis IgG(PV-IgG) in a passively transferred mouse model by inhibiting p38[7]. Inhibition of P38-MAPK by SB-202190(2.5µM/kg;24d; s.c.) resulted in increased primary tumor growth in tumor-bearing Balb-c mice (4T-1 cells) [8].
References:
[1]. Davies SP, Reddy H, et,al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. doi: 10.1042/0264-6021:3510095. PMID: 10998351; PMCID: PMC1221339.
[2]. Schwartz M, BÖckmann S, et,al.SB202190 inhibits endothelial cell apoptosis via induction of autophagy and heme oxygenase-1. Oncotarget. 2018 May 1;9(33):23149-23163. doi: 10.18632/oncotarget.25234. PMID: 29796178; PMCID: PMC5955409.
[3]. Grossi V, Liuzzi M, et,al.Sorafenib inhibits p38α activity in colorectal cancer cells and synergizes with the DFG-in inhibitor SB202190 to increase apoptotic response. Cancer Biol Ther. 2012 Dec;13(14):1471-81. doi: 10.4161/cbt.22254. Epub 2012 Sep 17. PMID: 22986232; PMCID: PMC3542239.
[4]. Nemoto S, Xiang J, et,al.Induction of apoptosis by SB202190 through inhibition of p38beta mitogen-activated protein kinase. J Biol Chem. 1998 Jun 26;273(26):16415-20. doi: 10.1074/jbc.273.26.16415. PMID: 9632706.
[5]. Muniyappa H, Das KC. Activation of c-Jun N-terminal kinase (JNK) by widely used specific p38 MAPK inhibitors SB202190 and SB203580: a MLK-3-MKK7-dependent mechanism. Cell Signal. 2008 Apr;20(4):675-83. doi: 10.1016/j.cellsig.2007.12.003. Epub 2007 Dec 8. PMID: 18222647; PMCID: PMC2423944.
[6]. Chen W, Tang Q, et,al.Role of p38 MAP kinases and ERK in mediating ultraviolet-B induced cyclooxygenase-2 gene expression in human keratinocytes. Oncogene. 2001 Jun 28;20(29):3921-6. doi: 10.1038/sj.onc.1204530. PMID: 11439356.
[7]. Berkowitz P, Hu P, et,al. p38MAPK inhibition prevents disease in pemphigus vulgaris mice. Proc Natl Acad Sci U S A. 2006 Aug 22;103(34):12855-60. doi: 10.1073/pnas.0602973103. Epub 2006 Aug 14. PMID: 16908851; PMCID: PMC1568937.
[8]. O'Sullivan AW, Wang JH, et,al. p38 MAP kinase inhibition promotes primary tumour growth via VEGF independent mechanism. World J Surg Oncol. 2009 Nov 15;7:89. doi: 10.1186/1477-7819-7-89. PMID: 19912664; PMCID: PMC2785811.
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