1. Apoptosis
  2. Caspase
  3. MX1013

MX1013 (Synonyms: CV1013; Z-VD-FMK)

Cat. No.: HY-10397A
Handling Instructions

MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM.

For research use only. We do not sell to patients.

MX1013 Chemical Structure

MX1013 Chemical Structure

CAS No. : 582316-00-5

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Description

MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM[1].

IC50 & Target[1]

Caspase

 

In Vitro

MX1013 inhibits caspases 1, 3, 6, 7, 8, and 9, with IC50 values ranging from 5 to 20 nm. MX1013 is selective for caspases, and is a poor inhibitor of noncaspase proteases, such as cathepsin B, calpain I, or Factor Xa (IC50 values >10 μm)[1].
MX1013 inhibits three key markers of apoptosis: the proteolytic maturation of caspase 3, the caspase-mediated cleavage of PARP, and the fragmentation of genomic DNA[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Jurkat T-lymphocytes
Concentration: 0, 0.05, 0.1, 0.25, 0.5 μM
Incubation Time: Preincubated for 2 h
Result: Neither caspase 3 processing nor PARP cleavage could be detected at 0.5 μM. At concentrations of 0.05 μM, caspase 3 processing and PARP cleavage were still markedly reduced.
In Vivo

MX1013 is an effective antiapoptotic agent in vivo. MX1013 not only inhibits local tissue apoptosis, but also can protect animals against its lethal effects[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female ND4 Swiss Webster mice (16.5-21 g)[1]
Dosage: 0, 0.25, 1, 10 mg/kg (formulated in an aqueous vehicle containing 50 mm Tris-HCl, pH 8.0)
Administration: Injected i.v.
Result: The lowest dose of 0.25 mg/kg protected 66% of the mice from the lethal effects of anti-Fas antibody at the 3 h time point, and 1 and 10 mg/kg dose protected 100% of the mice at the 3 h time point.
Molecular Weight

382.38

Formula

C18H23FN2O6

CAS No.
SMILES

O=C(O)CC(NC([[email protected]@H](NC(OCC1=CC=CC=C1)=O)C(C)C)=O)C(CF)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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MX1013
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