Z-VAD(OMe)-FMK NEW
Price | $52 | $147 | $247 |
Package | 1mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-04 |
Product Details
Product Name: Z-VAD(OMe)-FMK | CAS No.: 187389-52-2 |
Purity: 99.41% | Supply Ability: 10g |
Release date: 2024/11/04 |
Product Introduction
Bioactivity
名稱 | Z-VAD(OMe)-FMK |
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. |
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]. |
體外活性 | METHODS: Human leukemia cells HL60 were treated with Z-VAD(OMe)-FMK (50 μM) and camptothecin (50 M) for 3 h. Cell morphology was observed by electron microscopy. RESULTS: Cells treated with camptothecin exhibited typical apoptotic features including cell shrinkage, chromatin condensation and nuclear fragmentation.Z-VAD(OMe)-FMK combination treatment eliminated the camptothecin-induced apoptotic pattern. Z-VAD(OMe)-FMK alone did not affect cell morphology. [1] METHODS: Cholangiocarcinoma cells KKU100, KKU213A and KKU213B were pretreated with Z-VAD(OMe)-FMK (20 μM) for 1 h, followed by CH-MSCs (0%, 50% and 75%) for 24 h. Apoptosis was detected using Flow Cytometry. RESULTS: Z-VAD(OMe)-FMK pretreatment prevented the apoptosis induced by CH-MSCs. [2] METHODS: Human ovarian teratoma cells PA-1 were treated with Z-VAD(OMe)-FMK (50 μM) and UVB (100 J/m2) for 16 h, and the expression levels of target proteins were detected by Western Blot. RESULTS: Z-VAD(OMe)-FMK eliminated PARP cleavage induced by UVB. [3] |
體內(nèi)活性 | METHODS: To investigate whether in vivo administration of Z-VAD(OMe)-FMK prevents infection-induced preterm labor, a single intraperitoneal injection of Z-VAD(OMe)-FMK (10 mg/kg) was administered to CD1 mice in which preterm labor was induced by heat-killed group B streptococcus (HK-GBS). RESULTS: Z-VAD(OMe)-FMK pretreatment delayed but did not prevent HK-GBS-induced preterm labor in a pregnant mouse model. [4] METHODS: To prevent LPS-induced acute lung injury, Z-VAD(OMe)-FMK (0.25 mg 15 min before LPS stimulation, 0.1 mg three times per hour) was injected intravenously into ICR mice with LPS-induced apoptosis and acute lung injury. RESULTS: Z-VAD(OMe)-FMK inhibited caspase-3 activity in lung tissues. Z-VAD(OMe)-FMK significantly prolonged the survival of mice. Apoptosis may play an important role in acute lung injury, and thus inhibition of caspase activity may provide a new therapeutic approach for the treatment of this disease. [5] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 45 mg/mL (96.26 mM) |
關(guān)鍵字 | Inhibitor | ZVAD(OMe)FMK | inhibit | Caspase | Z-VAD(OMe)-FMK | Z VAD(OMe) FMK |
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相關(guān)庫 | 經(jīng)典已知活性庫 | 神經(jīng)退行性疾病化合物庫 | 蛋白酶抑制劑庫 | 多肽分子庫 | 抑制劑庫 | 已知活性化合物庫 | 共價抑制劑庫 | 含氟化合物庫 | 臨床前化合物庫 | 抗癌化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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