BIX02188

BIX02188 is a potent inhibitor of MEK5 (IC50 = 4.3 nM) with reduced activity towards inhibition of ERK5 and TGFbetaR1 (IC50s = 810 and 1,800 nM, respectively). It does not inhibit the closely related kinases MEK1, MEK2, ERK2, and JNK2 (IC50s = > 6,300 nM). BIX02188 inhibits phosphorylation of ERK5 in a dose-dependent manner without affecting phosphorylation of ERK1/2, p38 MAPK, or JNK1/2.Formal Name: (3Z)-3-[[[3-[(dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-2-oxo-1H-indole-6-carboxamide. CAS Number: 334949-59-6. Molecular Formula: C25H24N4O2. Formula Weight: 412.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. lambdamax: 210, 285, 384 nm. SMILES: CN(C)CC1=CC(N/C(C2=CC=CC=C2)=C3C(NC4=C\3C=CC(C(N)=O)=C4)=O)=CC=C1. InChi Code: InChI=1S/C25H24N4O2/c1-29(2)15-16-7-6-10-19(13-16)27-23(17-8-4-3-5-9-17)22-20-12-11-18(24(26)30)14-21(20)28-25(22)31/h3-14,27H,15H2,1-2H3,(H2,26,30)(H,28,31)/b23-22-. InChi Key: FSZPIAXLCCQFCM-FCQUAONHSA-N.