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Z-IETD-FMK Caspase-8 inhibitor

Catalog No.B3232
Size Price Stock Qty
10mM (in 1mL DMSO)
$820.00
In stock
1mg
$240.00
In stock
5mg
$350.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Tabtieng T, Degterev A, et al. "Caspase-dependent suppression of type I interferon signaling promotes KSHV lytic replication." J Virol. 2018 Mar 7. pii: JVI.00078-18. PMID:29514903
2. Dikchha Rijal. "Cell death signaling complexes during macrophage differentiation." University of Ottawa,2017.
3. Ardeshir Ariana,Faculty of Medicine, et al, "Dissection of TLR4-induced necroptosis using specific inhibitors of endocytosis and p38 MAPK." University of Ottawa, 2017.
4. Chen Y, Sun M, et al, "a novel PAC-1 derivative, activates procaspase-3 and causes cancer cell apoptosis." Cancer Chemother Pharmacol. 2016 Aug 3. PMID:27488460
5. Tian, Chongchong, et al. "A novel dual EGFR/HER2 inhibitor KU004 induces cell cycle arrest and apoptosis in HER2-overexpressing cancer cells." Apoptosis 20.12 (2015): 1599-1612. PMID:26437915

Quality Control

Chemical structure

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Related Biological Data

Z-IETD-FMK

Biological Activity

Description Z-IETD-FMK is a specific inhibitor of caspase 8
Targets caspase 8          
IC50            

Protocol

Cell experiment [1]:

Cell lines

Purified CD4+ and CD8+ T cells.

Preparation method

Limited solubility. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

24 h

Applications

T cell proliferation was assayed using [3H]-thymidine incorporation. z-IETD-FMK (100 μM) inhibits T cell proliferation. About 9% of control activated T cells took up PI after activation and in the presence of 100 μM of z-IETD-FMK cell death increases to 23%. In addition, 100 μM z-IETD-FMK decreases the nuclear translocation of p65 in activated T cells.

Animal experiment [2]:

Animal models

SHIP1-/- (CD45.1) mice

Dosage form

5 mg/kg three times each week for 3 weeks

Applications

There is a significant diminution of anatomical pathology in both the small intestine and lungs of Z-IETD-FMK-treated mice compared with vehicle-administered controls. There is also a prominent recovery of viable CD3+ T-cell numbers in small intestine and lung of the Z-IETD-FMK-treated SHIP1-/- hosts, whereas the vehicle-treated SHIP1-/- hosts exhibit the T-cell paucity.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Lawrence CP, Chow SC. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicol Appl Pharmacol. 2012 Nov 15;265(1):103-12.

2. Park MY, Srivastava N, Sudan R et al. Impaired T-cell survival promotes mucosal inflammatory disease in SHIP1-deficient mice. Mucosal Immunol. 2014 Nov;7(6):1429-39.

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Chemical Properties

Cas No. 210344-98-2 SDF Download SDF
Synonyms Benzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK
Chemical Name methyl 5-[[1-[(5-fluoro-1-methoxy-1,4-dioxopentan-3-yl)amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-[[3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate
Canonical SMILES CCC(C)C(C(=O)NC(CCC(=O)OC)C(=O)NC(C(C)O)C(=O)NC(CC(=O)OC)C(=O)CF)NC(=O)OCC1=CC=CC=C1
Formula C30H43FN4O11 M.Wt 654.68
Solubility >32.7mg/mL in DMSO Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Z-IETD-FMK is an inhibitor of caspase 8 [1].

Z-IETD-FMK inhibits T cell proliferation induced by PHA or anti-CD3 plus anti-CD28 without toxicity of resting T cells. The mechanism of this inhibition of Z-IETD-FMK has been proved not through the effect on IL-2 secretion or IFN-γ production but the decrease of CD25 expression. Experiments show that Z-IETD-FMK has no effect on normal cell growth when there is no activation signal. Z-IETD-FMK has also been found to significantly inhibit NF-κB activation when the concentration is 100μM [1].

Apart from the ability of inhibiting cell proliferation, Z-IETD-FMK is reported to inhibit TRAIL-mediated killing in cells. It protects the procaspases 9, 2, and 3, and protects PARP to a similar extent in both HCT116 and SW480 cells [2].

References:
[1] C.P. Lawrence, S.C. Chow. Suppression of human T cell proliferation by the caspase inhibitors, z-VAD-FMK and z-IETD-FMK is independent of their caspase inhibition properties. Toxicology and Applied Pharmacology. 2012, 265: 103-112.
[2] Nesrin Özören, Kunhong Kim, Timothy F. Burns, et al. The caspase 9 inhibitor Z-LEHD-FMK protects human liver cells while permitting death of cancer cells exposed to tumor necrosis factor-related apoptosis-inducing ligand. Cancer Research. 2000, 60: 6259-6265.