Ac-DEVD-CHO |
Catalog No.GC32695
One-Click Copy Product Info
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Ac-DEVD-CHO은 Caspase-3 억제제로서 IC50 값이 0.016μM이다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 169332-60-9
Sample solution is provided at 25 µL, 10mM.
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.
세포 실험[1]: | |
세포 라인 | OCLs |
제조 방법 | OCLs는 RANKL과 함께 푹 유동시키고, 특이성 반신경효소-3 억제제 Ac-DEVD-CHO(10μM)가 있거나 없는 상황에서 0.5 mmol/L의 SIN으로 24시간 처리되었다. |
반응 조건 | 10μM; 24 h |
응용 분야 | Ac-DEVD-CHO는 SIN 유도된 세포 자멸의 효과를 부분적으로 막았으며, 세포 자멸핵의 수를 감소시켰다. |
동물 실험 [2]: | |
동물 모형 | C3H 그리고 ICR 쥐 |
제조 방법 | 생후 8일부터 40마리의 C3H와 40마리의 ICR 새끼쥐는 2mg/kg 체중당 Ac-DEVD-CHO 또는 식염수를 배뇨로 투여했다. 그 중 각 그룹에서 10마리의 C3H와 ICR 쥐는 무작위로 선정되어 생후 13일에 살해되었으며, 각 그룹의 나머지 10마리의 C3H와 ICR 쥐는 17일에 사살하였다. |
제형 | 2mg/kg; i.p. |
응용 분야 | Ac-DEVD-CHO는 rd 유전자를 가진 C3H 쥐의 천식성 소뇌퇴행증 진행을 일시적으로 지연시킨다. |
참고문헌: [1] He L, Li X, Zeng X등.시노메닌은 caspase-3 활성화를 통해 in vitro에서 RAW 264.7세포 유래 조골세포에서 세포사멸을 유도한다 [J].Acta Pharmacologica Sinica, 2014, 35(2):203-210. [2] Yoshizawa K, Kiuchi K, Nambu H 등.Caspase-3억제제는 rd 유전자를 가지고 있는 C3H 생쥐에서 유전된 망막 변성을 전이적으로 지연시킨다 [J].Graefe's archive for clinical and experimental ophthalmology, 2002, 240:214-219. | |
| Cas No. | 169332-60-9 | SDF | |
| Canonical SMILES | N-Acetyl-Asp-Glu-Val-Asp-al | ||
| Formula | C20H30N4O11 | M.Wt | 502.47 |
| Solubility | Water : ≥ 50 mg/mL (99.51 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9902 mL | 9.9508 mL | 19.9017 mL |
| 5 mM | 398 μL | 1.9902 mL | 3.9803 mL |
| 10 mM | 199 μL | 995.1 μL | 1.9902 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)