BIX 02189

Description: BIX02189 is a novel, potent and selective inhibitor of MEK5 with important biological activity. It inhibits MEK5 with an IC50 of 1.5 nM. It also inhibits ERK5 with an IC50 of 59 nM in cell-free assays; but does not inhibit closely related kinases such as MEK1, MEK2, ERK2, and JNK2. BIX02189 was reported to inhibit catalytic function of purified, MEK5 enzyme. BIX02189 inhibited transcriptional activation of MEF2C, a downstream substrate of the MEK5/ERK5 signaling cascade, in a cellular trans-reporter assay system. BIX02189 may offer novel pharmacological tools to better characterize the role of the MEK5/ERK5 pathway in various biological systems.

References: Biochem Biophys Res Commun. 2008 Dec 5; 377(1):120-5; Circ Res. 2010 Mar 19; 106(5):961-70.

Related CAS: 1094614-85-3; 1265916-41-3

BIX 02189; BIX-02189; BIX02189

Chemical Name: (Z)-3-(((3-((dimethylamino)methyl)phenyl)amino)(phenyl)methylene)-N, N-dimethyl-2-oxoindoline-6-carboxamide

InChi Key: HOMJAAIVTDVQJA-IZHYLOQSSA-N

InChi Code: InChI=1S/C27H28N4O2/c1-30(2)17-18-9-8-12-21(15-18)28-25(19-10-6-5-7-11-19)24-22-14-13-20(27(33)31(3)4)16-23(22)29-26(24)32/h5-16, 28H, 17H2, 1-4H3, (H, 29, 32)/b25-24-

SMILES Code: O=C(C1=CC(NC/2=O)=C(C=C1)C2=C(NC3=CC=CC(CN(C)C)=C3)/C4=CC=CC=C4)N(C)C