A calpain and cathepsin inhibitor; inhibits µ-calpain and m-calpain (IC50s = 7.5 and 78 nM

Calpain Inhibitor VI – 1 mg

Brand:
Cayman
CAS:
190274-53-4
Storage:
-20
UN-No:
Non-Hazardous - /

Calpain inhibitor VI is an inhibitor of the calcium-dependent cysteine proteases µ-calpain (calpain-1; IC50 = 7.5 nM) and m-calpain (calpain-2; IC50 = 78 nM). It also inhibits cathepsins B and L (IC50s = 15 and 1.6 nM, respectively).{38603} It is selective for these calpains and cathepsins over other cysteine and serine proteases, factor VIIa, factor Xa, trypsin, chymotrypsin, and proteasome. In an in vitro porcine model of cataract, calpain inhibitor VI decreases the degree of cataract by 40% when used at a concentration of 0.8 µM.{38602} It also prevents cataract formation induced by selenite in rats when administered at a dose of 100 mg/kg for 4 days.{38604} Calpain inhibitor VI improves functional outcome and reduces apoptotic cell death in a rat model of spinal cord injury.{38601}  

 

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Description

A calpain and cathepsin inhibitor; inhibits µ-calpain and m-calpain (IC50s = 7.5 and 78 nM, respectively); inhibits cathepsin B and cathepsin L (IC50s = 15 and 1.6 nM, respectively); selective over other cysteine and serine proteases and several enzymes; effective in in vitro (0.8 µM) and in vivo (100 mg/kg per day for 4 days in rats) models of cataract

Formal name: 2S-[[(4-fluorophenyl)sulfonyl]amino]-N-[(1S)-1-formyl-3-methylbutyl]-3-methyl-butanamide

Synonyms:  SJA 6017

Molecular weight: 372.5

CAS: 190274-53-4

Purity: ≥95%

Formulation: A lyophilized solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Cell Biology|Proteolysis|Lysosomal Proteases||Research Area|Neuroscience|Ophthalmology

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