Home Apoptosis Caspase inhibitor Ac-DEVD-CHO

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Ac-DEVD-CHO Caspase inhibitor

Cat.No.S7901

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 Caspase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 502.47

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Quality Control

Batch: S790101 Water]100 mg/mL]false]]]false]]]false Purity: 98.86%
98.86

Chemical Information, Storage & Stability

Molecular Weight 502.47 Formula

C20H30N4O11

 Storage (From the date of receipt)
CAS No. 169332-60-9 Download SDF Storage of Stock Solutions

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

Solubility

In vitro
Batch:

Water : 100 mg/mL

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Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Caspase-3 [1]
(Cell-free assay)
230 pM(Ki)
caspase-8 [1]
(Cell-free assay)
0.92 nM(Ki)
caspase-7 [1]
(Cell-free assay)
1.6 nM(Ki)
caspase-10 [1]
(Cell-free assay)
12 nM(Ki)
Caspase-1 [1]
(Cell-free assay)
18 nM(Ki)
caspase-6 [1]
(Cell-free assay)
31 nM(Ki)
Caspase-9 [1]
(Cell-free assay)
60 nM(Ki)
Caspase-4 [1]
(Cell-free assay)
132 nM(Ki)
caspase-5 [1]
(Cell-free assay)
205 nM(Ki)
caspase-2 [1]
(Cell-free assay)
1.71 μM(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 compound (Ki = 1.7 μM). Group III caspases are broadly inhibited by this chemical with Ki values ranging from 1 to 300 nM[1]. Inhibition of caspase-3 by this inhibitor 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 this compound appear to be independent of apoptosis. Troponin I cleavage was not inhibited by this chemical[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]. This compound 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].
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24279384/
  • [5] https://www.jstage.jst.go.jp/article/ahc/36/4/36_4_263/_pdf

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