Ac-DEVD-CHO |
カタログ番号GC32695
One-Click Copy Product Info
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Ac-DEVD-CHOは、IC50値が0.016μMのカスパーゼ-3阻害剤である。
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-CHOは、IC50値が0.016μMのカスパーゼ-3阻害剤である。Ac-DEVD-CHOは他のカスパーゼファミリーのメンバーにも阻害活性を持つが、特にカスパーゼ-3に対して選択的であり、Ki値は0.23nMである。Ac-DEVD-CHOはカスパーゼの活性を阻害することによってアポトーシスプロセスを抑制し、アポトーシスプロセスや関連する疾患（例えば網膜変性）を研究するために使用できる。
In vitroでは、Ac-DEVD-CHO（10μM）がオステオクラス（OCL）を24時間処理し、シノメニン誘導アポトーシスを部分的に阻害し、アポトーシス核の数を減少させた。Ac-DEVD-CHO（100μM）が血管平滑筋細胞を48時間処理し、カスパーゼ-3の発現レベルを著しく減少させ、アルテスナート誘導アポトーシスを抑制した。
In vivoでは、Ac-DEVD-CHO（2mg/kg）が遺伝性網膜炎のマウスに腹腔内注射で投与され、視細胞のアポトーシスを効果的に抑制し、網膜変性を一時的に遅延させた。Ac-DEVD-CHO（4mg/kg）が急性腎障害のマウスに皮下投与され、血清BUN、TNF-α、IL-6、IL-10濃度および腎細胞アポトーシス率を著しく減少させた。
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.
細胞実験 [1]: | |
細胞株 | OCLs（オステオクラス） |
準備方法 | OCLsはRANKLで培養し、0.5 mmol/L SINを加えた後、特定のカスパーゼ-3阻害剤Ac-DEVD-CHO（10μM）を含むまたは含まない条件で24時間処理した。 |
反応条件 | 10μM; 24時間 |
アプリケーション | Ac-DEVD-CHOは、SIN誘導のアポトーシスの影響を部分的にブロックし、アポトーシス核の数を減少させた。 |
動物実験 [2]: | |
動物モデル | C3HおよびICRマウス |
準備方法 | 8日齢から始め、C3HおよびICRの子ネズミ40匹ずつに、体重2 mg/kgのAc-DEVD-CHOまたは生理食塩水を隔日で腹腔内注射した。各グループから10匹のC3HおよびICRマウスを13日齢で無作為に選択し、残りの10匹をそれぞれ17日齢で処理した。 |
投与形態 | 2mg/kg; 腹腔内注射 |
アプリケーション | Ac-DEVD-CHOは、C3Hマウスのrd遺伝子を保持するマウスで遺伝性網膜変性を一時的に遅延させる。 |
参考文献: [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. | |
| Cas No. | 169332-60-9 | SDF | |
| Canonical SMILES | N-Acetyl-Asp-Glu-Val-Asp-al | ||
| Formula | C20H30N4O11 | M.Wt | 502.47 |
| 溶解度 | 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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 39 reference(s) in Google Scholar.)