

HY-156193 · 5 mg
MedChemExpress · Cat: HY-156193
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medchemexpress.com/pf-07208254.htmlDescription
PF-07208254 is a selective, orally active allosteric inhibitor of branched-chain ketoacid dehydrogenase kinase BDK IC50=110 nM, Ki=54 nM, KD=84 nM . PF-07208254 inhibits BDK-mediated BCKDH phosphorylation and enhances the catabolism of branched-chain amino acids BCAAs and branched-chain keto acids BCKAs by binding to the allosteric pocket of BDK, reducing BDK binding to BCKDH-E2 and promoting BDK degradation. PF-07208254 inhibits BDK activity in human skeletal muscle cells IC50=540 nM and has activity to improve cardiac function and metabolism. PF-07208254 can be used in the study of cardiometabolic diseases e.g., heart failure, type 2 diabetes .







