Z-YVAD-FMK
目录号 : GC14188
Z-YVAD-FMK是一种可穿透细胞的不可逆caspase-1和caspase-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 cell-permeable, irreversible inhibitor of caspase‑1 and caspase‑4 [1]. Z‑YVAD‑FMK covalently binds to and blocks the activity of caspase‑1 and caspase‑4, inhibiting the maturation and release of downstream proinflammatory cytokines such as IL‑1β and IL‑18 [2-3]. Z‑YVAD‑FMK is commonly used to study inflammation and programmed cell death [4].
In Caco-2 cells, Inactivation of caspase-1 by Z-YVAD-FMK (100μM; 48h) abolishes butyrate-induced apoptosis [5]. In bone marrow-derived macrophages (BMDMs), Z-YVAD-FMK (100μM; 30min) treatment significantly reduced the percentage of propidium iodide-positive BMDMs, the release of lactate dehydrogenase, and IL-1β [6].
In ApoE−/− mice, the area of atherosclerotic lesions in aortic sections of mice treated with Z-YVAD-FMK (6.2mg/kg; ip; 4 weeks) was reduced by approximately 49.01% [6].
References:
[1]. Katsikis P D, Garcia-Ojeda M E, Torres-Roca J F, et al. Interleukin-1β converting enzyme–like protease involvement in Fas-induced and activation-induced peripheral blood T cell apoptosis in HIV infection. TNF-related apoptosis-inducing ligand can mediate activation-induced T cell death in HIV infection[J]. The Journal of experimental medicine, 1997, 186(8): 1365-1372.
[2]. Li H, Nookala S, Re F. Aluminum hydroxide adjuvants activate caspase-1 and induce IL-1β and IL-18 release[J]. The Journal of Immunology, 2007, 178(8): 5271-5276.
[3]. Bian Z M, Elner S G, Elner V M. Dual involvement of caspase-4 in inflammatory and ER stress-induced apoptotic responses in human retinal pigment epithelial cells[J]. Investigative ophthalmology & visual science, 2009, 50(12): 6006-6014.
[4]. Liu W, Yang D, Shi J, et al. Caspase-1 inhibitor reduces pyroptosis induced by brain death in kidney[J]. Frontiers in Surgery, 2021, 8: 760989.
[5]. 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]. The Journal of nutrition, 2002, 132(7): 1812-1818.
[6]. Zhang B L, Yu P, Su E Y, et al. Inhibition of GSDMD activation by Z-LLSD-FMK or Z-YVAD-FMK reduces vascular inflammation and atherosclerotic lesion development in ApoE−/− mice[J]. Frontiers in Pharmacology, 2023, 14: 1184588.
Z-YVAD-FMK是一种可穿透细胞的不可逆caspase-1和caspase-4 抑制剂 [1]。Z-YVAD-FMK与caspase-1和caspase-4共价结合并阻断其活性，从而抑制下游促炎细胞因子（如IL-1β和IL-18）的成熟和释放 [2-3]。Z-YVAD-FMK 常用于研究炎症和程序性细胞死亡 [4]。
在Caco-2细胞中，Z-YVAD-FMK（100μM；48h）抑制caspase-1可消除丁酸诱导的细胞凋亡 [5]。在骨髓来源的巨噬细胞（BMDM）中，Z-YVAD-FMK（100μM；30min）治疗显著降低了碘化丙啶阳性BMDM的百分比、乳酸脱氢酶和IL-1β的释放 [6]。
在ApoE-/-小鼠中，接受Z-YVAD-FMK（6.2mg/kg；ip；4周）治疗的小鼠主动脉切片中动脉粥样硬化病变面积减少了约49.01% [6]。
| Cell experiment [1]: | |
Cell lines | Caco-2 cells |
Preparation Method | Caco-2 cells were cultured in 24-multiwell plates to subconfluency and exposed to different butyrate concentrations (2, 5 or 10mM) and/or Z-YVAD-FMK (100μM) or Z-DVED-FMK (100μM) for 48h. |
Reaction Conditions | 100μM; 48h |
Applications | Inactivation of caspase-1 by Z-YVAD-FMK abolishes butyrate-induced apoptosis in Caco-2 cells. |
| Animal experiment [2]: | |
Animal models | ApoE−/− mice |
Preparation Method | Thirty-six 5-week-old ApoE−/− mice were also fed a Western diet and randomly divided into four groups at 14 weeks of age. Each group was treated with intraperitoneal injection for 4 weeks as follows: 1) control (vehicle, 0.25mL, 2% DMSO/day), 2) Z-YVAD-FMK (0.25 mL, 200μg/day), 3) Z-LLSD-FMK (0.25mL, 200μg/day), and 4) Z-YVAD-FMK + Z-LLSD-FMK (0.25mL, 200μg + 200μg/day). |
Dosage form | 6.2mg/kg; ip; 4 weeks |
Applications | The area of atherosclerotic lesions in aortic sections of mice treated with Z-YVAD-FMK was reduced by approximately 49.01%. |
References: | |
| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5855 mL | 7.9277 mL | 15.8554 mL |
| 5 mM | 317.1 μL | 1.5855 mL | 3.1711 mL |
| 10 mM | 158.6 μL | 792.8 μL | 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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