Ac-DEVD-CHO

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 K_i 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.