SB 202190 | CAS:152121-30-7

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Name:SB 202190; 
Cat. No. :CS-0141
CAS No. :152121-30-7
Formula:C20H14FN3O
M. Wt. : 331.34
Solubility:DMSO: ≥ 40 mg/mL

SB 202190 inhibits p38 and p38β2 with IC50 values of 50 nM and 100 nM. respectively.IC50 & Target: IC50: 50 nM (p38), 100 nM (p38β2)[1]In Vitro: Treatment of cells with SB 202190 (SB202190) significantly inhibits both basal and anti-Fas antibody-induced MAPKAPK 2 activity in a dose-dependent manner as measured in immune complex kinase assays with GST-hsp27 as a substrate. Jurkat cells are treated with SB202190 or left untreated. After 24 h, cells are harvested, and the activity of CPP32-like caspases in cell extracts is measured by cleavage of the fluorescent peptide DEVD-AMC, which is a specific substrate of CPP32-like caspases. The cleavage of DEVD-AMC is significantly increased in cells treated with SB202190 but not in the control[2].In Vivo: In HCT-116-derived colorectal tumors, administration of SB 202190 (SB202190), Sorafenib or a combination of both give similar results in terms of measurement of external tumor size (around 58% growth reduction compare with control tumors). SB202190 induces a 28% reduction of tumor growth, compare with a 31% reduction promoted by Sorafenib, while combination of both drugs reduce tumor growth by 55%[3]. Compare to the model group, the SB202190 group exhibits significantly shorter escape latencies in the Morris water maze hidden platform trials (P[4].

Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. Nemoto S, 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. Zhang Y, et al. PP2AC Level Determines Differential Programming of p38-TSC-mTOR Signaling and Therapeutic Response to p38-Targeted Therapy in Colorectal Cancer. EBioMedicine. 2015 Nov 19;2(12):1944-56. Yang S, et al. Protective effects of p38 MAPK inhibitor SB202190 against hippocampal apoptosis and spatial learning and memory deficits in a rat model of vascular dementia. Biomed Res Int. 2013;2013:215798. Grossi V, 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.