PF-07208254
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) [1][2].
Product Specifications
CAS Number
2573122-40-2
UNSPSC
12352005
Target
PDHK
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Neuroscience-Neuromodulation
Field of Research
Metabolic Disease; Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/pf-07208254.html
Purity
99.69
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
FC1=CC(SC(C(O)=O)=C2Cl)=C2S1
Molecular Formula
C7H2ClFO2S2
Molecular Weight
236.67
References & Citations
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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