Ac-Asp-Glu-Val-Asp-chloromethylketone trifluoroacetate salt

Names

[ Name ]:
Ac-Asp-Glu-Val-Asp-chloromethylketone trifluoroacetate salt

[Synonym ]:
L-Valinamide, N-acetyl-L-α-aspartyl-L-α-glutamyl-N-[(1S)-1-(carboxymethyl)-3-chloro-2-oxopropyl]-
N-Acetyl-L-α-aspartyl-L-α-glutamyl-N-[(2S)-1-carboxy-4-chloro-3-oxo-2-butanyl]-L-valinamide

Biological Activity

[Description]:

Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or 3,20-dibenzoate (IDB; HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis[1][2][3].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Signaling Pathways >> Apoptosis >> Caspase

Research Areas >> Metabolic Disease

[Target]

Caspase-3

[In Vitro]

Ac-DEVD-CMK (100 μM; 24 小时) 抑制 IDB 诱导的细胞凋亡[3]。 Apoptosis Analysis[3] Cell Line: Jurkat cells Concentration: 100 μM Incubation Time: 24 h Result: Inhibited ingenol IDB (10 μM)-induced apoptosis.

[In Vivo]

Ac-DEVD-CMK (Caspase-3 Inhibitor III; 25 mg/kg; 腹腔给药; 单剂量; APAP 后 3 小时) 显着减弱对乙酰氨基酚 (APAP; HY-66005) 诱导的肝损伤 (AILI)[4]。 Animal Model: 6- to 8-week-old females and males Sdc1-/- mice[4] Dosage: 25 mg/kg Administration: IP; single dose; 3 hours post-APAP Result: Significantly attenuated APAP (ip; 500 or 625 mg/kg)-induced liver injury (AILI), indicating that inhibition of GSK-3β or caspase-3 activity mitigates liver damage.

[References]

[1]. Lu Cai, et al. Hyperglycemia-induced apoptosis in mouse myocardium: mitochondrial cytochrome C-mediated caspase-3 activation pathway. Diabetes. 2002 Jun;51(6):1938-48.

[2]. M M Mocanu, et al. Caspase inhibition and limitation of myocardial infarct size: protection against lethal reperfusion injury. Br J Pharmacol. 2000 May;130(2):197-200.

[3]. M Blanco-Molina, et al. Ingenol esters induce apoptosis in Jurkat cells through an AP-1 and NF-kappaB independent pathway. Chem Biol. 2001 Aug;8(8):767-78.

[4]. Eon Jeong Nam, et al. Syndecan-1 limits the progression of liver injury and promotes liver repair in acetaminophen-induced liver injury in mice. Hepatology. 2017 Nov;66(5):1601-1615.