MX1013(Synonyms: CV1013; Z-VD-FMK)

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MX1013 (Synonyms: CV1013; Z-VD-FMK)

MX1013 是一种有效的、不可逆的二肽 caspase 抑制剂，具有抗细胞凋亡活性。MX1013 抑制重组人caspase 3，IC50为 30 nM。

MX1013(Synonyms: CV1013; Z-VD-FMK)

MX1013 Chemical Structure

CAS No. : 582316-00-5

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生物活性

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

 

体外研究
(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].

上海金畔生物科技有限公司 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.

体内研究
(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].

上海金畔生物科技有限公司 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.

分子量

382.38

Formula

C18H23FN2O6
CAS 号

582316-00-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [1]. Wu Yang, et al. MX1013, a dipeptide caspase inhibitor with potent in vivo antiapoptotic activity. Br J Pharmacol. 2003 Sep;140(2):402-12.

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