PD 151746

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PD 151746

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Cat No: 23417

Biochemicals - Small Molecule Inhibitors

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, an...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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

Correlated keywords:

PD151746 calpain 2m 1? Hep G2 HEK 293 hFPRL 1

Product Overview:
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}

Size	5 mg
Shipping	dry ice
CAS Number	179461-52-0
Molecular Formula	C₁₁H₈FNO₂S
SMILES	FC1=CC=C2C(C(/C=C(C(O)=O)\S)=CN2)=C1
Molecular Weight	237,2
Formulation	A crystalline solid
Purity	≥95%
Custom Code	2903.99
UNSPSC code	12352100

Technical File

MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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