1. Apoptosis
  2. Caspase
  3. Z-IETD-FMK

Z-IETD-FMK (Synonyms: Z-IE(OMe)TD(OMe)-FMK)

Cat. No.: HY-101297 Purity: >98.0%
Handling Instructions

Z-IETD-FMK is a selective and cell permeable caspase-8 and caspase-9 inhibitor.

For research use only. We do not sell to patients.

Z-IETD-FMK Chemical Structure

Z-IETD-FMK Chemical Structure

CAS No. : 210344-98-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 519 In-stock
Estimated Time of Arrival: December 31
1 mg USD 168 In-stock
Estimated Time of Arrival: December 31
5 mg USD 360 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Z-IETD-FMK purchased from MCE. Usage Cited in: Food Chem Toxicol. 2018 Oct;120:143-154.

    Z-IETD-FMK remarkably decreases the dioscin-induced up regulation of Caspase-3
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Z-IETD-FMK is a selective and cell permeable caspase-8 and caspase-9 inhibitor[1].

    IC50 & Target[1]

    Caspase-8

     

    Caspase-9

     

    In Vitro

    Z-IETD-FMK causes full inhibition only of the proapoptotic effect of TNFα with an IC50 of 0.46 μM[1]. Z-IETD-FMK and Z-VAD-FMK at non-toxic doses are found to be immunosuppressive and inhibit human T cell proliferation induced by mitogens and IL-2. They are shown to block NF-κB in activated primary T cells, but have little inhibitory effect on the secretion of IL-2 and IFN-γ during T cell activation[2]. Z-IETD-FMK inhibits the cleavage of caspase-8 and only partially inhibits the cleavage of caspase-3 and PARP. Z-IETD-FMK can prevent the execution of apoptosis in retinal cells exposed to different apoptotic stimuli[3].

    In Vivo

    Pharmacological inhibition of caspase-8 by z-IETD-FMK robustly reduces tumour outgrowth and this is closely associated with a reduction in the release of pro-inflammatory cytokines, IL-6, TNF-α, IL-18, IL-1α, IL-33, but not IL-1β. Furthermore, inhibition of caspase-8 reduces the recruitment of innate suppressive cells, such as myeloid-derived suppressor cells, but not of regulatory T cells to lungs of tumour-bearing mice[4].

    Molecular Weight

    654.68

    Formula

    C₃₀H₄₃FN₄O₁₁

    CAS No.

    210344-98-2

    Sequence

    Z-Ile-Glu-Thr-Asp-FMK

    Sequence Shortening

    ZIETDFMK

    SMILES

    O=C(N[[email protected]@H](CCC(OC)=O)C(N[[email protected]@H]([[email protected]](O)C)C(N[[email protected]](C(CF)=O)CC(OC)=O)=O)=O)[[email protected]]([[email protected]@H](C)CC)NC(OCC1=CC=CC=C1)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -80°C 2 years
      -20°C 1 year
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (190.93 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5275 mL 7.6373 mL 15.2746 mL
    5 mM 0.3055 mL 1.5275 mL 3.0549 mL
    10 mM 0.1527 mL 0.7637 mL 1.5275 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    • 2.

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

      Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (3.18 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [2]

    T cell proliferation following mitogen stimulation is determined using [3H]-thymidine incorporation. In brief, PBMCs or purified T cells are seeded at 1×106 cells/mL in 96 well plates and stimulated with either PHA (5 μg/mL or co-stimulated with anti-CD3 mAb (5 μg/mL) and anti-CD28 mAb (2.5 μg/mL) in the presence or absence of caspase inhibitor Z-IETD-FMK. The cells are cultured for 72 h with the last 16 h pulsed with [[3H]-labelled methyl-thymidine (0.037 MBq) prior to harvest onto glass fibre filter mats using a Tomtec automated multi-well harvester[2].

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

    Animal Administration
    [4]

    Mice: Mice are divided into three groups: (1) naive, non-treated, mice; (2) CTR (control), i.t. instilled with NMU; and (3) lung cancer-bearing mice treated with Z-IETD-FMK (0.5 μg per mouse). The involvement of caspase-8 in lung cancer development is the determined at different time points (3, 7 and 28 days)[4].

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

    References

    Purity: >98.0%

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    Keywords:

    Z-IETD-FMKZ-IE(OMe)TD(OMe)-FMKCaspaseInhibitorinhibitorinhibit

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    Product name:
    Z-IETD-FMK
    Cat. No.:
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