Ac-DEVD-CHO

製品コードS7901 バッチS790101

化学情報

	Synonyms	Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₃₀N₄O₁₁
	分子量	502.47	CAS No.	169332-60-9
Solubility (25°C)*	体外	Water	100 mg/mL (199.01 mM)


* <1 mg/ml means slightly soluble or insoluble. * 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	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.
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].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	MEFs
	濃度	20, 50 μM
	反応時間	2 h
	実験の流れ	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 this compound (0 μM).
動物実験	動物モデル	C57Bl6 mice
	投薬量	3 mg/kg
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/9829999/
https://pubmed.ncbi.nlm.nih.gov/11738316/
https://pubmed.ncbi.nlm.nih.gov/16966373/

https://pubmed.ncbi.nlm.nih.gov/24279384/
https://www.jstage.jst.go.jp/article/ahc/36/4/36_4_263/_pdf

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カスタマーフィードバック

: Data from [Data independently produced by , , Int J Oncol, 2018, 53(2):539-550]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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