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CAS No.: 169332-60-9

Ac-DEVD-CHO Catalog No. CSN23216

Synonyms: Caspase-3 Inhibitor I;N-Ac-Asp-Glu-Val-Asp-CHO

Ac-DEVD-CHO is a potent and specific Caspase-3 inhibitor with Ki of 230 pM.

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靶点选择性

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实验方案

技术信息

生物活性

描述Ac-DEVD-CHO is a highly potent peptide-base Group II caspase inhibitor, most potent to caspase 3 and caspase 8 with Ki value of 230pM and 920pM, respectively, and modest to caspase1/7/10/6/9 with Ki values of 18/1.6/12/31/60nM, and less potent to caspase 4/5/2 with Ki values of 132/205/1710nM^[1]^[2]. Ac-DEVD-CHO could inhibit the PARP cleavage activity in apoptotic osteosarcoma cells extract with IC50 of 0.2nM^[2]. Inhibition of caspase 3 through intraperitoneal injection with Ac-DEVD-CHO at dose of 3mg/kg for 3 days resulted in a reduction of activated caspase-3 by 61% and reduction of apoptosis by 84% in cardiomyocytes in young mice^[3].
作用机制DEVD is the canonical peptide sequence which can be recognized by Caspase-3 and caspase-7.^[4]
动物研究
剂量
Rat: 2 mg/kg^[5] (i.p.) Mice: 0.3 mg/kg - 3 mg/kg^[6] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Rat: 2 mg/kg^[5] (i.p.) Mice: 0.3 mg/kg - 3 mg/kg^[6] (p.o.)
给药途径	i.p., p.o.

[1] Garcia-Calvo M, Peterson EP, et al. Inhibition of human caspases by peptide-based and macromolecular inhibitors. J Biol Chem. 1998 Dec 4;273(49):32608-13.
[2] Nicholson DW, Ali A, et al. Identification and inhibition of the ICE/CED-3 protease necessary for mammalian apoptosis. Nature. 1995 Jul 6;376(6535):37-43.
[3] Boyle AJ, Hwang J, et al. The effects of aging on apoptosis following myocardial infarction. Cardiovasc Ther. 2013 Dec;31(6):e102-10.
[4] Fang B, Boross PI, et al. Structural and kinetic analysis of caspase-3 reveals role for s5 binding site in substrate recognition. J Mol Biol. 2006 Jul 14;360(3):654-66. Epub 2006 Jun 2.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9902 mL
- 9.9508 mL
- 19.9017 mL
- 5 mM
- 0.3980 mL
- 1.9902 mL
- 3.9803 mL
- 10 mM
- 0.1990 mL
- 0.9951 mL
- 1.9902 mL

技术信息

CAS号

169332-60-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H30N4O11

运输

蓝冰

分子量

502.47

别名

Caspase-3 Inhibitor I;N-Ac-Asp-Glu-Val-Asp-CHO

溶解度

DMSO	190.0 mg/mL (378.1 mM)
Water	175.0 mg/mL (348.3 mM)

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