Formaat : 5mg
Synonyms: Z-VAD(OH)-FMK, Caspase Inhibitor VI
| Description | Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM. |
| Targets & IC50 | Parasite growth:2.7 μM |
| In vitro | METHODS: Neutrophils were treated with Z-VAD-FMK (0.03-300 µM) for 30 min, then incubated with 200 U/mL TNFα for 6 h. Apoptosis was detected by Flow Cytometry. RESULTS: Z-VAD-FMK had a biphasic effect on TNFα-stimulated neutrophil apoptosis. 100 µM or more of Z-VAD-FMK enhanced TNFα-induced apoptosis, whereas 30 µM or less inhibited apoptosis. [1] METHODS: Human colorectal cancer cells HCT116 and SW480 were pretreated with Z-VAD-FMK (20 μM) for 1 h, then incubated with CPT (10-1000 ng/mL) and 5-FU (5-12.5 μg/mL) for 48 h to induce apoptosis, and then the expression levels of target proteins were detected by Western Blot. RESULTS: CPT and 5-FU induced significant up-regulation of cleaved caspase-3, caspase-8 and PARP, and Z-VAD-FMK pretreatment eliminated the activation of apoptosis-related proteins. [2] METHODS: Human T-lymphoblastic leukemia cells Jurkat were treated with Z-VAD-FMK (10-200 µM) for 24 h after pulsing, and cell viability was measured using propidium iodide. RESULTS: The optimal concentration of Z-VAD-FMK was 50 µM, which increased cell viability from 35% to 74% compared to untreated control. [3] |
| In vivo | METHODS: To detect anti-tumor activity in vivo, C57/BL6 mice bearing mouse melanoma tumor B16 were treated with RT (2 Gy local irradiation of the tumor on day 8/9/10), DTIC (2 mg/pc intraperitoneal injection on day 8/10), and a combination of Z-VAD-FMK (2 mg/kg intraperitoneal injection on day 8/9/10) and HT (4 h post-irradiation on day 8/10). RESULTS: Multimodal tumor therapy with RT, DTIC, and HT in combination with Z-VAD-FMK retarded tumor growth in a T-cell-dependent manner. [4] METHODS: To investigate the role of Z-VAD-FMK in endotoxin shock, Z-VAD-FMK (5-20 μg/g) was administered as a single intraperitoneal injection to LPS-induced endotoxin shock in C57BL/6 mice. RESULTS: Z-VAD-FMK treatment significantly prolonged the survival time of mice for several hours and increased the survival rate. Z-VAD-FMK treatment significantly reduced the mortality rate of mice treated with different doses of LPS. [5] |
| Synonyms | Z-VAD(OH)-FMK, Caspase Inhibitor VI |
| Molecular Weight | 453.46 |
| Formula | C21H28FN3O7 |
| Cas No. | 161401-82-7 |
| Smiles | CC(C)[C@H](NC(=O)OCc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(O)=O)C(=O)CF |
| Relative Density. | 1.260 g/cm3 (Predicted) |
| Sequence | Cbz-Val-Ala-Asp(OMe)-CH2F |
| Sequence Short | VAD |
| Storage | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 83 mg/mL (183.04 mM), Sonication is recommended. DMSO: 247.5 mg/mL (545.8 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 5% DMSO+95% Saline: 4.15 mg/mL (9.15 mM), Solution. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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