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MX1013
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MX1013图片
CAS NO:582316-00-5
包装与价格：
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
CV1013
Z-VD-FMK
产品介绍
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。
生物活性

MX1013 is a potent, irreversible dipeptidecaspaseinhibitor vith antiapoptotic activity. MX1013 inhibits recombinant humancaspase 3with anIC50 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].

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].

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

性状

Solid

Formula

C18H23FN2O6

CAS 号

582316-00-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month