Synonyms: (3Z)-3-[[[3-[(Dimethylamino)methyl]phenyl]amino]phenylmethylene]-2,3-dihydro-N,N-dimethyl-2-oxo-1H-indole-6-carboxamide; (Z)-3-((3-((Dimethylamino)methyl)phenylamino)(phenyl)methylene)-N,N-dimethyl-2-oxoindoline-6-carboxamide; BIX 02189; BIX-02189
Molecular Formula: C27H28N4O2
Molecular Weight: 440.54
Linear Structural Formula: C27H28N4O2
MDL Number: MFCD18074528
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: BIX02189 is an ATP site-targeting, potent and selective MEK5 inhibitor (IC50 =1.5 nM, [ATP] = 750 nM) with much reduced or no potency against 79 other kinases (CSF1R (FMS)/ERK5/Lck/Jak3/TGFβR1/RPS6KA6 (RSK4) IC50 = 46/59/250/440/580/990 nM, MEK1/MEK2/ERK2/JNK2/EGFR/STK16 IC50 >6.2 μM). BIX02189 blocks cellular ERK5, but not ERK1/2 or p38, phosphorylation induction (IC50<1 μm in sorbitol-stimulated hela), as well as downstream mef2c transcriptional activation (ic50="0.53/0.26" μm, mek5 rk5 ef2c hela ek293 reporter cells). bix02189 in vivo efficacies are demonstrated in murine models of atherosclerosis, cancer, and diabetes (10-20 mg g i.p.).<>