VER-246608

VER-246608 is a pan-inhibitor of pyruvate dehydrogenase kinase (PDHK, IC50s = 35, 84, 40, and 91 nM for PDHK1, -2, -3, and -4, respectively). It is selective for PDHKs over heat shock protein 90 (Hsp90, IC50 = >100 µM), as well as a panel of 97 kinases at 10 µM. VER-246608 (10 and 20 µM) decreases the production of L-lactate, a marker of glycolytic activity, in PC3 cells cultured in D-glucose- and L-glutamine-depleted media. It reduces the growth of, and induces cell cycle arrest at the G1 phase in, serum-starved PC3 cells when used at a concentration of 20 µM.Formal Name: N-[4-(2-chloro-5-methyl-4-pyrimidinyl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxy-benzamide. CAS Number: 1684386-71-7. Molecular Formula: C28H23ClF2N4O4. Formula Weight: 553.0. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2 mg/ml, DMSO: 2 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml. SMILES: OC1=CC(O)=C(C(N(C2=CC=C(C3=NC(Cl)=NC=C3C)C=C2)CC4=CC=C(CNC(C(F)F)=O)C=C4)=O)C=C1. InChi Code: InChI=1S/C28H23ClF2N4O4/c1-16-13-33-28(29)34-24(16)19-6-8-20(9-7-19)35(27(39)22-11-10-21(36)12-23(22)37)15-18-4-2-17(3-5-18)14-32-26(38)25(30)31/h2-13,25,36-37H,14-15H2,1H3,(H,32,38). InChi Key: LCGNLQSOSJFLKR-UHFFFAOYSA-N.