Z-DEVD-FMK
(Synonyms: CASPASE-3抑制剂,Caspase-3 Inhibitor II,Z-Asp(OMe)-Glu(OMe)-Val-Asp(OMe)-FMK) 目录号 : GC12287
Z-DEVD-FMK是一种特异性的不可逆的半胱氨酸-天冬氨酸蛋白酶3（caspase-3）抑制剂，IC50为18μM。
Cas No.:210344-95-9
Sample solution is provided at 25 µL, 10mM.
Z-DEVD-FMK is a specific irreversible cysteine-aspartic protease 3 (caspase-3) inhibitor with an IC50 of 18μM[1]. Z-DEVD-FMK is commonly used to study apoptosis and neuroprotection [2].
In vitro, Z-DEVD-FMK (50μM) treated cardiomyocytes for 24h, significantly reduced ceramide-induced apoptosis and increased cell survival rate to 81% [3]. Z-DEVD-FMK (15μM) can effectively reduce caspase-3 activity when treating renal proximal tubular cells, but the effect of reducing cell apoptosis is not as good as that of pan-caspase inhibitors [4].
In vivo, Z-DEVD-FMK (160 ng) treated mice with traumatic brain injury (TBI) via intracerebroventricular injection, reduced the lesion volume after central nervous system injury, and improved motor and cognitive functions [2]. Z-DEVD-FMK (20 mg/kg) treated diabetic mice via intraperitoneal injection for 8 weeks, which improved proteinuria, renal function, and tubulointerstitial fibrosis in mice, and slowed down the decrease in serum albumin levels [5] . Z-DEVD-FMK (0.2 mg/kg) is injected into the eyeball to treat optic nerve injury in rabbits, significantly reducing the apoptosis of retinal ganglion cells and promoting the recovery of optic nerve function [6].
References:
[1] Kanthasamy A G, Anantharam V, Zhang D, et al. A novel peptide inhibitor targeted to caspase-3 cleavage site of a proapoptotic kinase protein kinase C delta (PKCδ) protects against dopaminergic neuronal degeneration in Parkinson’s disease models[J]. Free Radical Biology and Medicine, 2006, 41(10): 1578-1589.
[2] Knoblach S M, Alroy D A, Nikolaeva M, et al. Caspase inhibitor z-DEVD-fmk attenuates calpain and necrotic cell death in vitro and after traumatic brain injury[J]. Journal of Cerebral Blood Flow & Metabolism, 2004, 24(10): 1119-1132.
[3] Wang J, Zhen L, Klug M G, et al. Involvement of caspase 3-and 8-like proteases in ceramide-induced apoptosis of cardiomyocytes[J]. Journal of cardiac failure, 2000, 6(3): 243-249.
[4] Yang B, El Nahas A M, Fisher M, et al. Inhibitors directed towards caspase-1 and-3 are less effective than pan caspase inhibition in preventing renal proximal tubular cell apoptosis[J]. Nephron Experimental Nephrology, 2004, 96(2): e39-e51.
[5] Wen S, Wang Z H, Zhang C X, et al. Caspase-3 promotes diabetic kidney disease through gasdermin E-mediated progression to secondary necrosis during apoptosis[J]. Diabetes, Metabolic Syndrome and Obesity, 2020: 313-323.
[6] Zhang W, Yu J G, Wang X, et al. Experimental study on treatment of rabbits optic nerve injury with Caspase-3 inhibitor z-DEVD-fmk[J]. [Zhonghua yan ke za Zhi] Chinese Journal of Ophthalmology, 2010, 46(12): 1084-1089.
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Cell experiment [1]: |
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Cell lines |
Cardiomyocytes |
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Preparation method |
Cardiomyocytes cultured in 6-well plates were treated with 75 mmol/L of ceramide in the presence of vehicle (DMSO) or 50μM of Z-DEVD-FMK. After 24 hours incubation, surviving cells from each well were counted. |
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Reaction Conditions |
50μM; 24 h |
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Applications |
Z-DEVD-FMK significantly reduced ceramide-induced cardiomyocyte apoptosis, increased cell survival rates to 81%. |
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Animal experiment [2]: |
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Animal models |
Male C57Bl/6 mice |
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Preparation method |
Mice underwent controlled cortical impact (CCI) followed by intracerebroventricular injection of Z-DEVD-FMK (160 ng). |
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Dosage form |
160 ng; i.c.v. |
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Applications |
Z-DEVD-FMK treatment reduced lesion volume after traumatic CNS injury induced by severe controlled cortical impact (CCI) in the mouse. |
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References: |
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| Cas No. | 210344-95-9 | SDF | |
| 别名 | CASPASE-3抑制剂,Caspase-3 Inhibitor II,Z-Asp(OMe)-Glu(OMe)-Val-Asp(OMe)-FMK | ||
| 化学名 | methyl (4S)-5-[[(2S)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-[[(2S)-4-methoxy-4-oxo-2-(phenylmethoxycarbonylamino)butanoyl]amino]-5-oxopentanoate | ||
| Canonical SMILES | CC(C)C(C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)C(CCC(=O)OC)NC(=O)C(CC(=O)OC)NC(=O)OCC1=CC=CC=C1 | ||
| 分子式 | C30H41N4O12F | 分子量 | 668.66 |
| 溶解度 | ≥ 60 mg/mL in DMSO | 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 | 1.4955 mL | 7.4776 mL | 14.9553 mL |
| 5 mM | 0.2991 mL | 1.4955 mL | 2.9911 mL |
| 10 mM | 0.1496 mL | 0.7478 mL | 1.4955 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: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
