Ac-DEVD-CHO is a Caspase-3 inhibitor with an IC50 value of 0.016μM[1]. Ac-DEVD-CHO also has inhibitory activity against other caspase family members, but is more selective for caspase-3, with a Ki value of 0.23nM [2]. Ac-DEVD-CHO inhibits the apoptosis process by inhibiting the activity of caspases, and can be used to study the apoptosis process and related diseases, such as retinal degeneration[3].
In vitro, Ac-DEVD-CHO (10μM) treated osteoclasts (OCLs) for 24 h, partially blocking sinomenine-induced apoptosis and reducing the number of apoptotic nuclei [4]. Ac-DEVD-CHO (100μM) treated vascular smooth muscle cells for 48 hours, significantly reducing the expression level of caspase-3 and inhibiting artesunate-induced apoptosis [5].
In vivo, Ac-DEVD-CHO (2mg/kg) treated mice with hereditary retinitis through intraperitoneal injection, effectively inhibiting photoreceptor cell apoptosis and temporarily delaying retinal degeneration[6]. Ac-DEVD-CHO (4mg/kg) was injected subcutaneously into mice with acute kidney injury and significantly reduced serum BUN, TNF-α, IL-6, IL-10 concentrations and renal cell apoptosis rate [7].
References:
[1] Firoozpour L, Gao L, Moghimi S, et al. Efficient synthesis, biological evaluation, and docking study of isatin based derivatives as caspase inhibitors[J]. Journal of enzyme inhibition and medicinal chemistry, 2020, 35(1): 1674-1684.
[2] Garcia-Calvo M, Peterson E P, Leiting B, et al. Inhibition of human caspases by peptide-based and macromolecular inhibitors[J]. Journal of Biological Chemistry, 1998, 273(49): 32608-32613.
[3] Yao K, Wang K, Xu W, et al. Caspase-3 and its inhibitor Ac-DEVD-CHO in rat lens epithelial cell apoptosis induced by hydrogen in vitro[J]. Chinese medical journal, 2003, 116(07): 1034-1038.
[4] He L, Li X, Zeng X, et al. Sinomenine induces apoptosis in RAW 264.7 cell-derived osteoclasts in vitro via caspase-3 activation[J]. Acta Pharmacologica Sinica, 2014, 35(2): 203-210.
[5] Zhang J, Wang L, Chen H, et al. Effect of Caspase Inhibitor Ac-DEVD-CHO on Apoptosis of Vascular Smooth Muscle Cells Induced by Artesunate[J]. AIMS Bioengineering, 2014, 1(1): 13-24.
[6] Yoshizawa K, Kiuchi K, Nambu H, et al. Caspase-3 inhibitor transiently delays inherited retinal degeneration in C3H mice carrying the rd gene[J]. Graefe's archive for clinical and experimental ophthalmology, 2002, 240: 214-219.
[7] Liu L X, Hu Z J, Li Y, et al. The effect of caspase-3 inhibitor on the concentrations of serum inflammatory cytokines in sepsis related acute kidney injury induced by peritoneal cavity infection in mice[J]. Zhongguo wei Zhong Bing ji jiu yi xue, 2010, 22(12): 736-739.
Ac-DEVD-CHO是一种Caspase-3抑制剂，IC50值为0.016μM[1]。Ac-DEVD-CHO对其他caspase家族成员的也有抑制活性，但对caspase-3的选择性更高，Ki 值为0.23nM[2]。Ac-DEVD-CHO通过抑制半胱天冬酶的活性，从而抑制细胞凋亡过程，可用于研究细胞凋亡过程及相关疾病，如视网膜变性[3]
在体外，Ac-DEVD-CHO（10μM）处理破骨细胞（OCLs）24 h，部分阻断了青藤碱诱导的细胞凋亡作用并减少了凋亡细胞核的数量[4]。Ac-DEVD-CHO（100μM）处理血管平滑肌细胞48h，显著降低了caspase-3的表达水平，抑制了青蒿琥酯诱导的细胞凋亡[5]。
在体内，Ac-DEVD-CHO（2mg/kg）通过腹腔注射治疗遗传性视网膜炎小鼠，有效抑制了感光细胞凋亡，可以短暂延缓视网膜变性[6]。Ac-DEVD-CHO（4mg/kg）通过皮下注射治疗急性肾损伤小鼠，显著降低了血清BUN、TNF-α、IL-6、IL-10浓度和肾细胞凋亡率[7]。