Chemical Structure : PF-07328948
CAS No.: 2936625-34-0
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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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.
分子量 | 356.29 | |
分子式 | C16H8F4O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
6-fluoro-3-(2,4,5-trifluoro-3-methoxyphenyl)benzo[b]thiophene-2-carboxylic acid |
1. Filipski KJ, et al. J Med Chem. 2024 Nov 19. doi: 10.1021/acs.jmedchem.4c02230.
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