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PF-07208254

Chemical Structure : PF-07208254

CAS No.: 2573122-40-2

PF-07208254 (PF 07208254)

Catalog No.: PC-21021Not For Human Use, Lab Use Only.

PF-07208254 (PF 07208254) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with in vitro IC50 of 110 nM and Ki of 54 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

PF-07208254 (PF 07208254) is a potent, allosteric branched-chain ketoacid dehydrogenase kinase (BDK) 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.

Physicochemical Properties

M.Wt 236.66
Formula C7H2ClFO2S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

3-chloro-5-fluorothieno[3,2-b]thiophene-2-carboxylic acid

References

1. Rachel J Roth Flach, et al. Nat Commun. 2023 Aug 9;14(1):4812.

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