Z-YVAD-FMK
目录号 : GC14188
Z-YVAD-FMK 是一种具有抗炎和抗肿瘤活性的细胞渗透性 caspase-1 和 -4 抑制剂。
Cas No.:210344-97-1
Sample solution is provided at 25 µL, 10mM.
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Z-YVAD-FMK is a potent cell-permeable and irreversible inhibitor of caspase-1.
In Caco-2 cells, Z-YVAD-FMK significantly decreased the growth inhibition induced by butyrate. Complete abrogation of butyrate’s effect occurred at an inhibitor concentration of 100 mol/L. It is indicated that caspase-1 inhibitor significantly alters the caspase cascade, diminishing the butyrate-induced apoptotic effect [1]. After treated with Alum reflected caspase-1 activation, IL-1-release in cells was blocked by Z-YVAD-FMK. This effect was observed even in MyD88-deficient bone marrow DC [2].
References:
1.Avivi-Green C, Polak-Charcon S, Madar Z, et al. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines. J Nutr. 2002 Jul;132(7):1812-8.
2.Li H, Nookala S, Re F. Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1beta and IL-18 release. J Immunol. 2007 Apr 15;178(8):5271-6.
| Cell experiment [1]: | |
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Cell lines |
Caco-2 (ATCC Number HTB-37) |
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Preparation method |
Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reaction Conditions |
48 h |
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Applications |
Z-YVAD-FMK significantly downregulates the growth inhibition induced by butyrate in Caco-2 Cells. Complete abrogation of butyrate’s effect occurs at an inhibitor concentration of 100 μmol/L, indicating that caspase-1 inhibitor significantly alters the caspase cascade, diminishing the butyrate-induced apoptotic effect. |
| Animal experiment [2]: | |
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Animal models |
Albino Wistar rats |
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Dosage form |
Rats were injected intravenously (2 μL) with caspase inhibitor Z-VAD-FMK (1.06 mM in 2% DMSO) |
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Applications |
Immediately before exposure to damaging light, YVAD significantly reduces caspase-1 activity to 51% ± 34% but has no effect on caspase-3 activity (98% ± 5%). Exposed-YVAD retinas showed caspase-1 activities of 66% ± 33%, respectively. These values were significantly (P < 0.02 and P < 0.004, respectively) lower than in the Exposed-DMSO group. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Avivi-Green C, Polak-Charcon S, Madar Z, Schwartz B. Different molecular events account for butyrate-induced apoptosis in two human colon cancer cell lines. J Nutr. 2002 Jul;132(7):1812-8. 2. Perche O, Doly M, Ranchon-Cole I. Caspase-dependent apoptosis in light-induced retinal degeneration. Invest Ophthalmol Vis Sci. 2007 Jun;48(6):2753-9. |
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| Cas No. | 210344-97-1 | SDF | |
| 化学名 | (8S,11S,14S)-methyl 14-(2-fluoroacetyl)-5-(4-hydroxybenzyl)-8-isopropyl-11-methyl-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,10,13-tetraazahexadecan-16-oate | ||
| Canonical SMILES | COC(C[C@H](NC([C@H](C)NC([C@@H](NC(C(CC1=CC=C(O)C=C1)NC(OCC2=CC=CC=C2)=O)=O)C(C)C)=O)=O)C(CF)=O)=O | ||
| 分子式 | C31H39FN4O9 | 分子量 | 630.7 |
| 溶解度 | ≥ 31.55mg/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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5855 mL | 7.9277 mL | 15.8554 mL |
| 5 mM | 0.3171 mL | 1.5855 mL | 3.1711 mL |
| 10 mM | 0.1586 mL | 0.7928 mL | 1.5855 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