Chemical Structure : PF-07208254
CAS No.: 2573122-40-2
Catalog No.: PC-21021Not For Human Use, Lab Use Only.
PF-07208254 (PF 07208254) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK, BCKDK) inhibitor with in vitro IC50 of 110 nM and Ki of 54 nM.
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PF-07208254 (PF 07208254) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK, BCKDK) inhibitor with in vitro IC50 of 110 nM and Ki of 54 nM.
PF-07208254 exhibits potent inhibitory potency in human skeletal myocytes using an AlphaLISA SureFire Ultra detection system to monitor BCKDH phosphorylation (cellular IC50 = 540 nM).
PF-07208254 exhibits Kd value of 84 nM in surface plasmon resonance (SPR)-based binding assays.
PF-07208254 demonstrates superior potency relative to BT2 (Cat. PC-49378, IC50=1100 nM in vitro).
PF-07208254 (90 mg/kg) improves cardiac function and metabolism, reduces pBCKDH in mice.
PF-07208254 reduces pBCKDH and promotes BDK protein levels in human cells and in mice.
M.Wt | 236.66 | |
Formula | C7H2ClFO2S2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
3-chloro-5-fluorothieno[3,2-b]thiophene-2-carboxylic acid |
1. Rachel J Roth Flach, et al. Nat Commun. 2023 Aug 9;14(1):4812.
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