PDHK1-IN-1

PDHK1-IN-1 (compound 17) is a selective inhibitor of PDHK1 (IC50=1.5 μM) with anticancer activity. PDHK1 negatively regulates the pyruvate dehydrogenase complex (PDC), limiting the tricarboxylic acid (TCA) cycle and oxidative phosphorylation. Overexpression of PDHK1 can shift the metabolism towards an increased glycolysis dependence (Warburg effect) . PDHK1-IN-1 can inhibit the phosphorylation of the PDC E1α Ser232 recognition site of PDHK1 and the phosphorylation of Ser293[1].

C14H11BrClNO4S

404.66

ClC1=CC=C(C(S(=O)(NC2=C(C=CC(C(O)=O)=C2)Br)=O)=C1)C

PDHK

Room temperature