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PF-07208254

CAT: 0804-HY-156193-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-156193-01Size:5 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
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].
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
[1]Roth Flach RJ, et al. Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels. Nat Commun. 2023 Aug 9;14 (1) :4812.|[2]Filipski KJ, et al. Discovery of First Branched-Chain Ketoacid Dehydrogenase Kinase (BDK) Inhibitor Clinical Candidate PF-07328948. J Med Chem. 2025 Feb 13;68 (3) :2466-2482.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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