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PF-07328948

Chemical Structure : PF-07328948

CAS No.: 2936625-34-0

PF-07328948 (PF07328948)

货号: PC-23451Not For Human Use, Lab Use Only.

PF-07328948 is the first potent, selective branched-chain ketoacid dehydrogenase kinase (BDK or BCKDK) with in vitro IC50 of 15 nM, and cellular IC50 of 46 nM in human skeletal muscle BDK activity assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PF-07328948 is the first potent, selective branched-chain ketoacid dehydrogenase kinase (BDK or BCKDK) with in vitro IC50 of 15 nM, and cellular IC50 of 46 nM in human skeletal muscle BDK activity assay.
PF-07328948 is not only a BDK inhibitor but also BDK degrader.
PF-07328948 shows a high degree of selectivity over a number of enzymes, receptors, and ion channels, as well as excellent kinase selectivity.
PF-07328948 binds to the BDK allosteric pocket and does not contain a traditional ATP-binding site motif.
PF-07328948 binds to BDK with SPR Kd of 4.8 nM.
PF-07328948 also destabilizes the interaction between BDK and E2.
PF-07328948 also shows high species potency against mouse BDK IC50 = 41 nM, rat BDK IC50 = 24 nM, and dog BDK IC50 = 24 nM. lowered plasma biomarkers, including BCAAs and branched-chain ketoacids (BCKAs) in vivo with enhanced pharmacodynamic effect upon chronic dosing due to BDK degradation.

物理化学性质&存储条件

分子量 356.29
分子式 C16H8F4O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-fluoro-3-(2,4,5-trifluoro-3-methoxyphenyl)benzo[b]thiophene-2-carboxylic acid

参考文献

1. Filipski KJ, et al. J Med Chem. 2024 Nov 19. doi: 10.1021/acs.jmedchem.4c02230.

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