Z-VAD-FMK

Catalog No.S7023 Batch:S702304

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Technical Data

Formula

C22H30FN3O7

Molecular Weight 467.49 CAS No. 187389-52-2
Solubility (25°C)* In vitro DMSO 93 mg/mL (198.93 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.
Targets
Pan-caspase [1]
(THP.1, Jurkat T-cells)
In vitro

Z-VAD-FMK (10 μM) inhibits apoptosis in THP.1 cells. Z-VAD-FMK (10 μM) inhibits activation of PARP protease activity in control THP.1 cell lysates. Z-VAD-FMK (10 μM) inhibits the processing of CPP32 in intact THP.1 and Jurkat cells. [1] Z-VAD-FMK (50 μM) cotreatment abolishes the apoptotic morphology of camptothecin-treated HL60 cells. Z-VAD-FMK (50 μM) blocks camptothecin-induced DNA fragmentation in HL60 cells. [2] Z-VAD-FMK (50 μM) inhibits cell death following dSMN dsRNA-induced apoptosis in S2 cells. Z-VAD-FMK (50 μM) increases the percentage of transfected cells surviving from 26% to 63% in S2 cells. [3] Z-VAD-FMK (> 100 μM) enhances TNFα-induced neutrophil apoptosis, lower concentrations (1-30 μM) completely blocks TNFα-stimulated apoptosis in human neutrophils. [4] Z-VAD-FMK (10 mM) inhibits apoptosis in anterior stromal keratocytes. Z-VAD-FMK (10 mM) inhibits apoptosis in anterior stromal keratocytes detected with the TUNEL assay. [5]

In vivo

In vivo Z-VAD-FMK administration has been shown previously to be nontoxic and to prevent apoptosis in animal models. Intraperitoneal HK-GBS injection leads to preterm delivery, and pretreatment with Z-VAD-FMK delays preterm delivery in mice. In OVA-sensitized mice,treatment of z-VAD-fmk inhibits allergen-induced leukocyte infiltration. Systemic injection of the pan-caspase inhibitor z-VAD-fmk immediately before OVA challenge reduced inflammatory cell accumulation, mucus hypersecretion, and Th2 cytokine release in OVA-sensitized/challenged mice. Treatment with z-VAD-fmk blocked terminal differentiation of lens epithelial cells and keratinocytes, the differentiation of monocytes into macrophages, and the differentiation of erythroid progenitors. z-VAD-fmk attenuated allergen-induced airway inflammation and hyperreactivity. Treatment with z-VAD-fmk in vivo also prevented subsequent T cell activation ex vivo[7].

Features A key compound for apoptosis studies.

Protocol (from reference)

Cell Assay:

[6]

  • Cell lines

    human granulosa cell lines (GC1a, HGL5, COV434)

  • Concentrations

    50 μM

  • Incubation Time

    48 h

  • Method

    To validate the efficacy of Z-VAD-FMK, three human granulosa cell lines (GC1a, HGL5, COV434) were treated for 48 h under normoxic conditions. To mimic the ischemic phase that occurs after ovarian fragment transplantation, cells were cultured without serum under hypoxia (1 % O2) and treated with Z-VAD-FMK. The metabolic activity of the cells was evaluated by WST-1 assay. Cell viability was determined by FACS analyses. The expression of apoptosis-related molecules was assessed by RT-qPCR and Western blot analyses.

Animal Study:

[7]

  • Animal Models

    CD1 mice

  • Dosages

    10 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Acta Pharmacol Sin, 2014, 35(4):531-9]

Data from [Data independently produced by , , Science, 2018, 10(441), doi: 10.1126/scitranslmed.aao4680]

Data from [Data independently produced by , , Cancer Res, 2017, 77(4):926-936]

Data from [Data independently produced by , , Theranostics, 2017, 7(15):3690-3699]

Selleck's Z-VAD-FMK has been cited by 1190 publications

7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] PubMed: 38297130
7-Dehydrocholesterol dictates ferroptosis sensitivity [ Nature, 2024, 626(7998):411-418.] PubMed: 38297130
NLRC5 senses NAD+ depletion, forming a PANoptosome and driving PANoptosis and inflammation [ Cell, 2024, 187(15):4061-4077.e17] PubMed: 38878777
Combined targeting of GPX4 and BCR-ABL tyrosine kinase selectively compromises BCR-ABL+ leukemia stem cells [ Mol Cancer, 2024, 23(1):240] PubMed: 39465372
CircPIAS1 promotes hepatocellular carcinoma progression by inhibiting ferroptosis via the miR-455-3p/NUPR1/FTH1 axis [ Mol Cancer, 2024, 23(1):113] PubMed: 38802795
SLC13A3 is a major effector downstream of activated β-catenin in liver cancer pathogenesis [ Nat Commun, 2024, 15(1):7522] PubMed: 39215042
Plasticity-induced repression of Irf6 underlies acquired resistance to cancer immunotherapy in pancreatic ductal adenocarcinoma [ Nat Commun, 2024, 15(1):1532] PubMed: 38378697
Oncogenic EML4-ALK assemblies suppress growth factor perception and modulate drug tolerance [ Nat Commun, 2024, 15(1):9473] PubMed: 39488530
EFHD2 suppresses intestinal inflammation by blocking intestinal epithelial cell TNFR1 internalization and cell death [ Nat Commun, 2024, 15(1):1282] PubMed: 38346956
The Toxoplasma Effector GRA4 Hijacks Host TBK1 to Oppositely Regulate Anti-T. Gondii Immunity and Tumor Immunotherapy [ Adv Sci (Weinh), 2024, 11(32):e2400952] PubMed: 39031880

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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