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Z-VAD(OMe)-FMK 是一种具有不可逆特性的pan-caspase抑制剂。Z-VAD(OMe)-FMK 还是泛素 C 端水解酶 L1 (UCHL1) 的抑制剂,它通过靶向 UCHL1 活性位点进行不可逆修饰。
Z-VAD(OMe)-FMK 是一种具有不可逆特性的pan-caspase抑制剂。Z-VAD(OMe)-FMK 还是泛素 C 端水解酶 L1 (UCHL1) 的抑制剂,它通过靶向 UCHL1 活性位点进行不可逆修饰。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 538 | 现货 | |
5 mg | ¥ 1,390 | 现货 | |
10 mg | ¥ 2,230 | 现货 | |
25 mg | ¥ 3,570 | 现货 | |
50 mg | ¥ 4,890 | 现货 | |
100 mg | ¥ 6,790 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,450 | 现货 |
产品描述 | Z-VAD(OMe)-FMK is a pan-caspase inhibitor with irreversible properties; Z-VAD(OMe)-FMK is also an inhibitor of ubiquitin C terminal hydrolase L1 (UCHL1), which is irreversibly modified by targeting the UCHL1 active site. |
体外活性 | 方法:人白血病细胞 HL60 用 Z-VAD(OMe)-FMK (50 µM) 和 camptothecin (150 μM) 处理 3 h,使用电子显微镜观察细胞形态。
结果:用 camptothecin 处理的细胞表现出典型的凋亡特征包括细胞收缩、染色质浓缩和核碎裂。Z-VAD(OMe)-FMK 联合治疗消除了 camptothecin 诱导的细胞凋亡形态。单独的 Z-VAD(OMe)-FMK 不影响细胞形态。[1] 方法:胆管癌细胞 KKU100、KKU213A 和 KKU213B 用 Z-VAD(OMe)-FMK (20 µM) 预处理 1 h,随后用 CH-CM (0%、50% 和 75%)处理 24 h,使用 Flow Cytometry 方法检测细胞凋亡情况。 结果:Z-VAD(OMe)-FMK 预处理阻止了 CH-MSCs 诱导的细胞凋亡。[2] 方法:人卵巢畸胎瘤细胞 PA-1 用 Z-VAD(OMe)-FMK (50 μM) 和 UVB (100 J/m2) 处理 16 h,使用 Western Blot 方法检测靶点蛋白表达水平。 结果:Z-VAD(OMe)-FMK 消除了 UVB 引起的 PARP切割。[3] |
体内活性 | 方法:为研究 Z-VAD(OMe)-FMK 的体内给药是否能预防感染诱导的早产,将 Z-VAD(OMe)-FMK (10 mg/kg) 单次腹腔注射给用热致死的 B 组链球菌 (HK-GBS) 诱导早产的 CD1 小鼠。
结果:Z-VAD(OMe)-FMK 预处理延迟但不能阻止 HK-GBS 在妊娠小鼠模型中诱导的早产。[4] 方法:为防止 LPS 引起的急性肺损伤,将 Z-VAD(OMe)-FMK (LPS 刺激前 15 分钟,0.25 mg;每小时三次,0.1 mg) 静脉注射给 LPS 诱导凋亡和急性肺损伤的 ICR 小鼠。 结果:Z-VAD(OMe)-FMK 抑制了肺组织中的 caspase-3 活性。Z-VAD(OMe)-FMK 可显著延长小鼠的存活率。细胞凋亡可能在急性肺损伤中发挥重要作用,因此抑制 caspase 活性可能为治疗该疾病提供一种新的治疗方法。[5] |
细胞实验 | The human monocytic tumour cell line, THP.1 and the leukaemic T-cell line, Jurkat (clone E-6) were maintained in RPMI 1640 supplemented with 10% (v/v) heat-inactivated fetal calf serum, 100 units/ml penicillin and 100 μg/ml streptomycin in an atmosphere of 5% CO2 in air at 37 °C. The cells were maintained in logarithmic growth phase by routine passage every 2–3 days. To induce apoptosis in THP.1 cells, 2×10^6 cells/ml were incubated either alone or in the presence of cycloheximide (25 μM) and TLCK (100 μM) as previously described. In order to assess the possible effects of various ICE-like protease inhibitors, THP.1 cells were also pretreated for 1 h with Z-VAD.FMK (10 μM), Ac-DEVD-CHO (20 μM) and Ac-YVAD-CHO (20 μM) before being exposed to the apoptotic stimulus. To induce apoptosis in Jurkat cells, 2×10^6 cells/ml were stimulated with 200 ng/ml anti-human Fas as described previously [1]. |
动物实验 | Mice used in this study were 5- to 6-week-old (20 to 22 g) ICR males. Mice were injected with 30 mg/kg LPS from E. coli serotype O111:B4 through the tail vein. Z-VAD.fmk was dissolved at 2 mg/ml in 1% dimethyl sulfoxide in sterile saline, and administered to mice by the method of Rodriguez et al. A single intravenous injection of Z-VAD.fmk (0.25 mg) was made 15 minutes before LPS injection, followed by three intravenous injections of Z-VAD.fmk (0.1 mg each) per hour. Control mice were injected with the same volume of 1% DMSO in sterile saline [4]. |
别名 | Z-VAD-FMK, Z-Val-Ala-Asp(OMe)-FMK |
分子量 | 467.49 |
分子式 | C22H30FN3O7 |
CAS No. | 187389-52-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 45 mg/mL (96.26 mM) | ||||||||||||||||||||||||||||||
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DMSO
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