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> Z-VAD-FMK [161401-82-7]

Z-VAD-FMK [161401-82-7]

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Referencia HY-16658B-1mL

embalaje : 10mM/1mL

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Descripciòn

Z-VAD-FMK is a pan-caspase inhibitor and also an ICE-like protease inhibitor, which inhibits apoptosis by preventing the processing of CPP32 to its active form. Z-VAD-FMK sensitivity varies primarily due to differential expression of receptor-interacting protein 1 (RIP1). Z-VAD-FMK limits the cryopreservation-induced apoptosis by reducing caspase-3 activity of in vitro produced bovine embryos. Z-VAD-FMK is immunosuppressive in vitro and inhibits T cell proliferation without blocking the processing of caspase-8 and caspase-3. Z-VAD-FMK leads to a decrease in intracellular glutathione (GSH) with a concomitant increase in reactive oxygen species (ROS) levels in activated T cells. Z-VAD-FMK is due to oxidative stress via the depletion of GSH. Z-VAD-FMK can be used for the study of acute pancreatitis[1][2][3][4][5][6][7].

IC50 & Target[1]

Caspase

 

In Vitro

Z-VAD-FMK (100 μM, 8 h) can induce both autophagy and necrosis in J774A.1 macrophages, indicating that it can trigger non-apoptotic cell death pathways[2].
Z-VAD-FMK (20 μM, 48 h) significantly improves the cryotolerance of Bovine in vitro produced blastocysts by inhibiting apoptosis, and improves the survival and development of embryos after thawing[3].
Z-VAD-FMK (20 μM, 48 h) directly inhibits caspase-3 activation, demonstrating that it improves the cryotolerance of bovine blastocysts by blocking the apoptosis pathway[3].
Z-VAD-FMK (0-100 μM, 72 h) dose-dependently inhibits T cell proliferation mediated through the co-stimulation with anti-CD3 and anti-CD28[4].
Z-VAD-FMK (50-100 μM, 16 h) significantly inhibits FasL-induced T cell apoptosis and caspase-8/caspase-3 treatment[4].
Z-VAD-FMK (25-100 μM, 6-24 h) can deplete and activate GSH in anti-CD3 antibody-pretreated peripheral blood mononuclear cells (PBMCs) following prolonged incubation[5].
Z-VAD-FMK (25-100 μM, 6-24 h) significantly increases ROS levels in primary T cells[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Z-VAD-FMK Related Antibodies

Western Blot Analysis[4]

Cell Line: FasL-induced T cells
Concentration: 50 μM, 100 μM
Incubation Time: 16 h
Result: Effectively inhibited caspase activity in the apoptosis model, but had no effect on T cell activation.
In Vivo

Z-VAD-FMK (3 mg/kg, i.p., once every other day, for 3 months) can reduce inflammation and mucus secretion in mice induced by cigarette smoke[6].
Z-VAD-FMK (50 μmol/L (0.3 mL), i.p., 30 mins before modeling) significantly reduces severe acute pancreatitis (SAP)-induced lung tissue pathological damage in a SAP model in rats[7].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Thirty-two 6-7-week-old male C57BL/6J mice were exposed to cigarette smoke (CS)[6].
Dosage: 3 mg/kg
Administration: I.P., once every other day, for 3 months
Result: Significantly reduced airway inflammation and emphysema lesions caused by CS exposure.
Lowered serum IL-1β, IL-8, and IL-1β levels in BALF.
Had no significant inhibitory effect on mucus secretion (Muc5ac).
Animal Model: Seventy-two male Sprague-Dawley rats (weighing 250-300 g) were anesthetized by intraperitoneal injection of ketamine (100 mg/kg), followed by laparotomy and retrograde injection of 5% sodium taurocholate (1.0 mL/kg) into the pancreatic duct via the duodenal papilla[7].
Dosage: 50 μmol/L (0.3 mL)
Administration: I.p., 30 mins before modeling
Result: Significantly alleviated SAP-induced pathological damage to lung tissue (edema, inflammatory infiltration, and hemorrhage).
Inhibiting cleaved caspase-3 expression blocked lung cell apoptosis.
Reduced myeloperoxidase (MPO) activity and inflammatory cytokine (IL-1β, TNF-α) levels, inhibiting neutrophil infiltration and inflammatory responses.
Peso molecular

453.46

Fòrmula

C21H28FN3O7
No. CAS
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N[C@H](C(N[C@@H](C)C(N[C@@H](CC(O)=O)C(CF)=O)=O)=O)C(C)C)OCC1=CC=CC=C1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvente y solubilidad
In Vitro: 

DMSO : 100 mg/mL (220.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2053 mL 11.0263 mL 22.0527 mL
5 mM 0.4411 mL 2.2053 mL 4.4105 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.59 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.59 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Pureza y Documentación
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