Ac-DEVD-CHO

Catalog No.S7901 Synonyms: Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO

For research use only.

Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.

Ac-DEVD-CHO Chemical Structure

CAS No. 169332-60-9

Selleck's Ac-DEVD-CHO has been cited by 19 publications

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Biological Activity

Description Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.
Targets
Caspase-3 [1]
(Cell-free assay)
caspase-8 [1]
(Cell-free assay)
caspase-7 [1]
(Cell-free assay)
caspase-10 [1]
(Cell-free assay)
Caspase-1 [1]
(Cell-free assay)
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230 pM(Ki) 0.92 nM(Ki) 1.6 nM(Ki) 12 nM(Ki) 18 nM(Ki)
In vitro

Ac-DEVD-CHO is a potent inhibitor of caspase-3 (Ki = 230 pM). In contrast, caspase-2 cleaves the tetrapeptide substrate poorly and is only weakly inhibited by this aldehyde (Ki = 1.7 μM). Group III caspases are broadly inhibited by Ac-DEVD-CHO with Ki values ranging from 1 to 300 nM[1]. Inhibition of caspase-3 by Ac-DEVD-CHO in isolated working-heart rat model significantly improves post-ischemic contractile recovery of stunned myocardium, even when given after the onset of ischemia. The mechanism(s) of protection by Ac-DEVD-CHO appear to be independent of apoptosis. Troponin I cleavage was not inhibited by Ac-DEVD-CHO[2].

In vivo Ac-DEVD-CHO administered at the time of MI results in a 61% reduction in activated caspase-3 expression in cardiomyocytes (p<0.05), and an 84% reduction in cardiomyocyte apoptosis in the young animals. However, in the aging mice, caspase inhibition had no effect on activated caspase-3 expression or cardiomyocyte apoptosis[4]. Ac-DEVD-CHO suppressed and/or delayed the progression of photoreceptor cell damage in rats and delays disease progression in rd gene-carring mice, which normally develop retinal degeneration early in life[2].

Protocol (from reference)

Cell Research:

[3]

  • Cell lines: MEFs
  • Concentrations: 20, 50 μM
  • Incubation Time: 2 h
  • Method:

    Apaf-1−/− cells were treated with the indicated concentration of Ac-DEVD-CHO for 2 h prior to treatment with 4 μM CHX alone or with TNF for 6 h. LEHDase and DEVDase activities were standardized to the lactate dehydrogenase activity in the sample and are presented as percentages of the activity in TNF-plus-CHX-treated cells not treated with Ac-DEVD-CHO (0 μM).

Animal Research:

[4]

  • Animal Models: C57Bl6 mice
  • Dosages: 3 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 502.47
Formula

C20H30N4O11

CAS No. 169332-60-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C(C(=O)NC(CC(=O)O)C=O)NC(=O)C(CCC(=O)O)NC(=O)C(CC(=O)O)NC(=O)C

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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