Z-DEVD-FMK

Catalog No.S7312 Synonyms: Caspase-3 Inhibitor

Z-DEVD-FMK Chemical Structure

Molecular Weight(MW): 668.66

Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

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3 Customer Reviews

  • Immunoblotting analysis was performed for the active-caspase-3 and cleavage of MCL-1 in MM.1S cells treated with z-DEVD-fmk (20 μM, 1 h) and following GSK126 (25 μM, 24 h).

    Oncotarget, 2017, 8(2):3396-3411. Z-DEVD-FMK purchased from Selleck.

    (J,K)After pre-treated with Caspase-3 inhibitor Z-DEVD-FMK 50μM, the apoptotic rates of cells induced by E Platinum in BGC-823, MGC-803, and SGC-7901 cells were detected by Annexin V/PI double-staining assay. Ann.V-/PI- as healthy cells, Ann.+/PI- as early apoptotic cells, Ann.+/PI+ probably as late apoptotic cells. Data were shown as means SD for three independent experiments (*P<0.05 and **P<0.01 compared with control, ##P<0.01 compared to Z-DEVD-FMK+40 μM E Platinum group with treatment of 40 μM E Platinum).

    Mol Carcinog, 2016, 56(1):218-231. Z-DEVD-FMK purchased from Selleck.

  • Caspase activation degrades Beclin-1. (A and B) After pretreatment with z-VAD-fmk (20 μM) or z-DEVD-fmk (20 μM) for 1 h, K562 cells were exposed to BIIB021 (400 nM) while 32Dp210-T315I cells were exposed to BIIB021 (200 nM) for 24 h. Whole-cell lysates were subjected to western blot analysis to examine the expression of Beclin-1, LC3I/II, p62, PARP and caspase-3.

    INTERNATIONAL JOURNAL OF ONCOLOGY, 2016, 48:1710-1720.. Z-DEVD-FMK purchased from Selleck.

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Biological Activity

Description Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.
Targets
Caspase-3 [1]
In vitro

Z-DEVD-FMK (1–200 μM) inhibits D4-GDI cleavage and apoptosis in a concentration-dependent manner. [1] Z-DEVD-FMK reduces ceramide-induced cardiomyocyte death and significantly inhibits the activation of caspase 3. [3] Z-DEVD-FMK (100μM) attenuates OxyHb-induced cell detachment, reduced caspase-2 and -3 activities, abolishes OxyHb-induced DNA ladders, and prevents OxyHb-induced cleavage of PARP in cultured brain microvessel endothelial cells. [4] Z-DEVD-FMK (100 μM) blocks MPP+-induced increases in caspase-3 enzyme activity. Z-DEVD-FMK dose dependently blocks 6-OHDA-induced apoptotic cell death with IC50 of 18 μM. [5]

In vivo Z-DEVD-FMK, before and after injury, markedly reduces post-traumatic apoptosis, and significantly improved neurological recovery. [2]

Protocol

Kinase Assay:[5]
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Caspase activity assay :

Caspase-3 and caspase-9 activities are measured using fluorescent-based substrate. After treatment, the cells are resuspended in lysis buffer (50 mM Tris HCl, 1 mM EDTA, and 10 mM EGTA) containing 10 mM digitonin for 20 min at 37°C. Supernatants are treated with either of the fluorogenic substrates Ac-DEVD-AFC for caspase-3 or Ac-LEHD-AFC for caspase-9 for 1 h at 37°C and fluorescence is measured at excitation at 400 nm and emission at 505 nm using a Gemini XS fluorescence plate reade
Cell Research:[5]
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  • Cell lines: N27 cells
  • Concentrations: ~50 μM
  • Incubation Time: 24 hours
  • Method: N27 cells are incubated with 100 μM 6-OHDA for 24 h or 300 μM MPP+ for 36 h in the presence or absence of 50 μM Z-DEVD-FMK and cell death is determined by MTT (3-(4,5-dimethylthiazol-3-yl)-2,5-diphenyl tetrazolium bromide) assay, which is widely used to assess cell viability. After treatment, the cells are incubated in serum-free medium containing 0.25 mg/ml MTT for 3 h at 37°C. Formation of formazan from tetrazolium is measured at 570 nm with a reference wavelength at 630 nm using a SpectraMax microplate reader.
    (Only for Reference)
Animal Research:[2]
+ Expand
  • Animal Models: Male Sprague Dawley rats with Brain trauma.
  • Formulation: DMSO
  • Dosages: 160 ng
  • Administration: Intracerebroventricular administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (149.55 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 400+5% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/mL

* 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.

Chemical Information

Molecular Weight 668.66
Formula

C30H41FN4O12

CAS No. 210344-95-9
Storage powder
Synonyms Caspase-3 Inhibitor

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID