| Bioactivity | 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]. |
| Target | EC50: 19 nM (BCKDC kinase, BDK) |
| Invitro | PF-07238025 (0.2-6 μM；48 h) 在 Hek293 细胞中以剂量依赖性方式降低 pBCKDH，并使 BDK 积累增加 50%[1]。 0 --> PF-07238025 相关抗体: |
| In Vivo | PF-07238025（20 mg/kg、100 mg/kg；8 周）在 HFD 喂养小鼠，2 天后可降低血糖波动，并在第 7 天时导致 BCAA 和 BCKA 水平显着降低[1]。 |
| Name | PF-07238025 |
| Formula | C19H18N2O3S |
| Molar Mass | 354.42 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |