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Ac-DEVD-CHO

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Chemical Structure| 169332-60-9 同义名 : Caspase-3 Inhibitor I;N-Ac-Asp-Glu-Val-Asp-CHO
CAS号 : 169332-60-9
货号 : A426528
分子式 : C20H30N4O11
纯度 : 98%+
分子量 : 502.472
MDL号 : MFCD00671412
存储条件：

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

液体 -20°C:1个月-80°C:12个月
溶解度 :

H2O: 50 mg/mL(99.51 mM)
动物实验配方：
生物活性
靶点

  • Caspase-4

    Caspase-4, Ki:132 nM

  • Caspase-3

    Caspase-3, Ki:230 pM

  • Caspase-8

    caspase-8, Ki:0.92 nM

  • Caspase-5

    caspase-5, Ki:205 nM
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]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.95mL

1.99mL

1.00mL

19.90mL

3.98mL

1.99mL
参考文献

[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.