Ac-DEVD-CHO
目录号 : GC32695
Ac-DEVD-CHO是一种Caspase-3抑制剂，IC50值为0.016μM。
Cas No.:169332-60-9
Sample solution is provided at 25 µL, 10mM.
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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]。
Cell experiment [1]: | |
Cell lines | OCLs |
Preparation method | OCLs were incubated with RANKL and treated with 0.5 mmol/L SIN with or without the specific caspase-3 inhibitor Ac-DEVD-CHO (10μM) for 24 h. |
Reaction Conditions | 10μM; 24 h |
Applications | Ac-DEVD-CHO partially blocked the effect of SIN-induced apoptosis and reduced the number of apoptotic nuclei. |
Animal experiment [2]: | |
Animal models | C3H and ICR mice |
Preparation method | Starting at 8 days of age, 40 C3H and 40 ICR pups received an i.p. injection of 2 mg/kg body weight of Ac-DEVD-CHO or saline every other day.Ten C3H and ICR mice per group were randomly selected and killed at 13 days of age, and the remaining 10 C3H and ICR mice in each group were killed at 17 days. |
Dosage form | 2mg/kg; i.p. |
Applications | Ac-DEVD-CHO transiently delays inherited retinal degeneration in C3H mice carrying the rd gene. |
References: [1] 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. [2] 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. | |
| Cas No. | 169332-60-9 | SDF | |
| Canonical SMILES | N-Acetyl-Asp-Glu-Val-Asp-al | ||
| 分子式 | C20H30N4O11 | 分子量 | 502.47 |
| 溶解度 | Water : ≥ 50 mg/mL (99.51 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9902 mL | 9.9508 mL | 19.9017 mL |
| 5 mM | 0.398 mL | 1.9902 mL | 3.9803 mL |
| 10 mM | 0.199 mL | 0.9951 mL | 1.9902 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet