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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
50 mM
0.0398 mL
0.1990 mL
0.3980 mL
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 values of 0.2 nM and 0.3 nM for for and , respectively. Weak inhibition for caspase-2.
Targets
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. 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.
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. 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.