A substrate-selective p38α MAPK inhibitor
CMPD1 is a selective and non-ATP-competitive p38 MAPK-mediated MK2 phosphorylation inhibitor with apparent Ki (Kiapp) of 330?nM[1][2].
CMPD1 does not inhibit p38 MAPK-mediated phosphorylation of other two substrates, MBP and ATF2[1].CMPD1 induced mitotic arrest and apoptosis in U87 cells[1].CMPD1 inhibits tubulin polymerisation in glioblastoma cells[3].
参考文献:
[1]. Gurgis F, et al. Cytotoxic activity of the MK2 inhibitor CMPD1 in glioblastoma cells is independent of MK2. Cell Death Discov. 2015 Sep 7;1:15028.
[2]. Davidson W, er al. Discovery and characterization of a substrate selective p38alpha inhibitor. Biochemistry. 2004 Sep 21;43(37):11658-71.
[3]. Phoa AF, et al. Pharmacology of novel small-molecule tubulin inhibitors in glioblastoma cells with enhanced EGFR signalling. Biochem Pharmacol. 2015 Dec 15;98(4):587-601.
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