BIX02189

BIX02189 is a potent inhibitor of both MEK5 and ERK5 (IC50s = 1.5 and 59 nM, respectively), preventing transcriptional activation of the downstream target MEF2C. It minimally inhibits a panel of related kinases, including MEK1/2 and ERK1/2. BIX02189 blocks sorbitol-induced phosphorylation of ERK5, without affecting phosphorylation of ERK1/2, in HeLa cells. It has been used to investigate the roles of MEK5/ERK5 signaling in nerve growth factor-mediated neurite outgrowth and myeloid cell differentiation.Formal Name: (3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide. CAS Number: 1265916-41-3. Molecular Formula: C27H28N4O2. Formula Weight: 440.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 10 mg/ml, Ethanol: 10 mg/ml. lambdamax: 284, 385 nm. SMILES: CN(C)CC1=CC(N/C(C2=CC=CC=C2)=C3C(NC4=C\3C=CC(C(N(C)C)=O)=C4)=O)=CC=C1. 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-. InChi Key: HOMJAAIVTDVQJA-IZHYLOQSSA-N.