Z-VAD(OMe)-FMK
作者：齊岳
發布時間：2023-08-28
09:04:41
點擊數：
產品名稱：Z-VAD(OMe)-FMK
產品描述：
| 產品描述 | Z-VAD(OMe)-FMK is a cell-permeable and irreversible pan-caspase inhibitor. It inhibits cleavage of PARP, preventing apoptosis when used at 10-50 μM. | ||||||||||||||||
| 體外活性 | Z-VAD.FMK was a poor inhibitor of PARP protease activity in cell lysates. Z-VAD.FMK (10 μM) is a potent inhibitor of Fas-induced apoptosis [1]. CPP32 is activated during camptothecin-induced apoptosis, and Z-VAD-fmk blocks all features of apoptosis. However, Z-VAD-fmk is inactive in a cell-free system reconstituted from nuclei of untreated HL60 cells and cytosol from camptothecin-treated cells [2]. z-VAD-FMK suppressed TUNEL and caspase-3 staining in endothelial cells, decreased caspase-3 activation, reduced BBB permeability, relieved vasospasm, abolished brain edema, and improved neurological outcome [3].
| ||||||||||||||||
| 體內活性 | LPS (30 mg/kg) was administered intravenously to Institute for Cancer Research mice. Z-VAD.fmk was injected before and after the administration of LPS. The injection of Z-VAD.fmk suppressed the caspase-3 activity in lung tissues and significantly decreased the number of terminal dUTP nick-end labeling-positive cells [4]. Treatment with the specific caspase inhibitor Z-VAD-FMK (i.p.) prior to heat-killed group B streptococcus (i.p.) delayed but did not prevent preterm delivery [5].
| ||||||||||||||||
| 細胞實驗 | 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]. | ||||||||||||||||
| 動物實驗 | 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]. |
| 別名 | Z-Val-Ala-Asp(OMe)-FMK, Z-VAD-FMK |
| 化合物與蛋白結合的復合物 |
Crystal structure of the SARS-CoV-2 main protease in complex with Z-VAD(OMe)-FMK |
| 分子量 | 467.494 |
| 分子式 | C22H30FN3O7 |
| CAS No. | 187389-52-2 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 93 mg/mL (198.93 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
聯系我們：
郵箱：2519696869@qq.com
QQ: 2519696869
電話：18066853083
微信：18066853083
公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
主營產品：COF、MOF單體系列：三蝶烯衍生物、金剛烷衍生物、四苯甲烷衍生物、peg、上轉換、石墨烯、光電材料、點擊化學、凝集素、載玻片、蛋白質交聯劑、脂質體、蛋白、多肽、氨基酸、糖化學等。
