PF-07238025

PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM) . PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice[1].

Product Specifications

UNSPSC

12352005

Target

Endogenous Metabolite

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pf-07238025.html

Purity

99.46

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CC(C)COC(N=C1)=CC=C1C2=NC(C3=CC=CC=C3C(O)=O)=CS2

Molecular Formula

C19H18N2O3S

Molecular Weight

354.42

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.