Ac-DEVD-CHO |
| Catalog No.GC32695 |
Ac-DEVD-CHO은 Caspase-3 억제제로서 IC50 값이 0.016μM이다.
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Cas No.: 169332-60-9
Sample solution is provided at 25 µL, 10mM.
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Ac-DEVD-CHO은 Caspase-3 억제제로서 IC50 값이 0.016μM이다.
Ac-DEVD-CHO은 다른 caspase 가족 구성원에도 억제 작용이 있지만, caspase-3에 대해 더 선택적이며, Ki 값이 0.23nM이다[2]. Ac-DEVD-CHO는 caspases의 활동을 억제하여 조기 세포 사멸 과정을 억제하고 반대 시력 감퇴 등 조기 세포 사멸 과정 및 관련 질병을 연구하는 데 사용될 수 있다[3].
체외 실험에서, Ac-DEVD-CHO(10μM)는 24시간 동안 osteoclasts (OCLs)를 처리하여 sinomenine 유도한 조기 세포사멸을 부분적으로 차단하고 조기 세포사멸핵의 수를 줄였다[4]. Ac-DEVD-CHO(100μM)는 48시간 동안 혈관 원활 근세포를 처리하여 caspase-3의 표현 수준을 현저하게 낮추고 아르테수산 유도 조기 세포사멸을 억제했다[5].
체내 실험에서 복강 주사로 Ac-DEVD-CHO(2mg/kg)를 투여하여 유전성 반시망성 환자 쥐를 치료하고, 광피질세포의 조기 세포사멸을 효과적으로 억제하고 반시망성의 진행을 일시적으로 지연시켰다[6]. Ac-DEVD-CHO(4mg/kg)는 쥐의 급성 신부전에 피하 주사하여혈청 BUN, TNF-α, IL-6, IL-10 농도와 신장세포 조기 세포사멸률을 현저하게 낮추었다[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.
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