Ac-DEVD-CHO

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

Ac-DEVD-CHO Chemical Structure

Molecular Weight(MW): 502.47

Ac-DEVD-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.

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Biological Activity

Description Ac-DEVD-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)
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

Cell Research:

[3]
+ Expand
  • 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).


    (Only for Reference)
Animal Research:

[4]
+ Expand
  • Animal Models: C57Bl6 mice
  • Formulation: --
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (199.01 mM)
 
 

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 502.47
Formula

C20H30N4O11
CAS No. 169332-60-9
Storage powder
in solvent
Synonyms Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID