An inhibitor of calpain 1 (Ki = 0.26 µM); 20-fold selective for calpain 1 over calpain 2 (Ki = 5.33 µM); selective over cathepsin B

PD 151746 – 5 mg

Brand:
Cayman
CAS:
179461-52-0
Storage:
-20
UN-No:
Non-Hazardous - /

PD 151746 is an inhibitor of calpain 1/μ-calpain (Ki = 0.26 µM).{22460} It is 20-fold selective for calpain 1 over calpain 2/m-calpain (Ki = 5.33 µM). It is also selective over cathepsin B, papain, trypsin, and thermolysin, (Kis = >200, >500, >500, and >500 µM, respectively) and does not inhibit basal calcineurin activity (Ki = >200 µM) but does inhibit calmodulin-induced calcineurin activity (Ki = 84.54 µM). It reduces glycogen synthesis induced by insulin in HepG2 cells when used at a concentration of 5.33 µM.{47217} PD 151746 (10 µM) also increases intracellular calcium in isolated human neutrophils and HEK293 cells expressing human formyl peptide receptor-like 1 (hFPRL1).{47218}  

 

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Description

An inhibitor of calpain 1 (Ki = 0.26 µM); 20-fold selective for calpain 1 over calpain 2 (Ki = 5.33 µM); selective over cathepsin B, papain, trypsin, and thermolysin, (Kis = >200, >500, >500, and >500 µM, respectively); does not inhibit basal calcineurin activity (Ki = >200 µM) but does inhibit calmodulin-induced calcineurin activity (Ki = 84.54 µM); increases intracellular calcium in isolated human neutrophils and HEK293 cells expressing hFPRL1 at 10 µM

Formal name: 3-(5-fluoro-1H-indol-3-yl)-2-mercapto-2-propenoic acid

Synonyms: 

Molecular weight: 237.2

CAS: 179461-52-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes

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