DMX-5084

A MAP4K4 inhibitor (IC50 = 3 nM), selective for MAP4K4 over a panel of 141 kinases at 1 µM but does inhibit MAP4K6 and TNIK (IC50s = 6.61 and 10.96 nM, respectively), prevents hydrogen peroxide-induced decreases in viability in vCor.4U cells (EC50 = 3.16 nM), inhibits menadione-induced decreases in the OCR and ECAR in vCor.4U cells at 3 or 10 µM, prevents menadione-induced decreases in the number of beats per minute and force of contraction in a 3D hEHT model using vCor.4U cells, reduces infarct size in a mouse model of ischemia-reperfusion injury induced by LAD coronary artery occlusion at 50 mg/kg. Formulation: A solid. InChI: InChI=1S/C21H19N3O3/c1-26-11-12-27-17-9-7-15(8-10-17)18-13-24(16-5-3-2-4-6-16)20-19(18)21(25)23-14-22-20/h2-10,13-14H,11-12H2,1H3,(H,22,23,25). InChIKey: FUSHFOGORKZNNQ-UHFFFAOYSA-N. SMILES: O=C1N=CNC2=C1C(C3=CC=C(OCCOC)C=C3)=CN2C4=CC=CC=C4