A dipeptide pan-caspase inhibitor; inhibits caspase-1 (IC50 = 20 nM)

MX1013 – 5 mg

Brand:
Cayman
CAS:
582316-00-5
Storage:
-20
UN-No:
Non-Hazardous - /

MX1013 is a dipeptide pan-caspase inhibitor that inhibits caspase-1 (IC50 = 20 nM), caspase-3 (IC50 = 30 nM), and caspase-6, -7, -8, and -9 (IC50s = 5-18 nM).{42697} It is selective for caspases over calpain I, cathepsin B, cathepsin D, renin, thrombin, and Factor Xa (IC50s = >10 μM). MX1013 (0.05 μM) inhibits anti-Fas antibody-induced caspase-3 processing and poly(ADP)ribose polymerase (PARP) cleavage in Jurkat cells, indicating inhibition of apoptosis. It increases survival in a mouse model of anti-Fas antibody-induced liver failure when administered at doses of greater than or equal to 0.25 mg/kg. MX1013 reduces infarct size in rat models of acute myocardial infarction-reperfusion or transient focal brain ischemia-reperfusion injury when administered intravenously as a 20 mg/kg bolus dose followed by a 5 mg/kg per hour infusion.  

 

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SKU: 27904 - 5 mg Category:

Description

A dipeptide pan-caspase inhibitor; inhibits caspase-1 (IC50 = 20 nM), caspase-3 (IC50 = 30 nM), and caspase-6, -7, -8, and -9 (IC50s = 5-18 nM); selective for caspases over calpain I, cathepsin B, cathepsin D, renin, thrombin, and Factor Xa (IC50s = >10 μM); inhibits anti-Fas antibody-induced caspase-3 processing and PARP cleavage in Jurkat cells at 0.05 μM; increases survival in a mouse model of anti-Fas antibody-induced liver failure at ≥0.25 mg/kg; reduces infarct size in rat models of acute myocardial infarction-reperfusion or transient focal brain ischemia-reperfusion injury intravenously as a 20 mg/kg bolus dose followed by a 5 mg/kg per hour infusion

Formal name: 5-fluoro-3-[[(2S)-3-methyl-1-oxo-2-[[(phenylmethoxy)carbonyl]amino]butyl]amino]-4-oxo-pentanoic acid

Synonyms:  Z-Val-Asp-Fluoromethyl Ketone|Z-VD-FMK

Molecular weight: 382.4

CAS: 582316-00-5

Purity: ≥98%

Formulation: A solid

Product Type|Biochemicals|Small Molecule Inhibitors|Caspases||Research Area|Cardiovascular System|Cardiovascular Diseases|Myocardial Infarction||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Neuroscience|Neuroprotection|Ischemia

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