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Z-IETD-FMK

In stock
Catalog No.
B3232
Caspase-8 inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$820.00
In stock
20 µl (10 mM)
$125.00
In stock
100 µl (2 mM)
$125.00
In stock
1mg
$240.00
In stock
5mg
$350.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

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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.

Product Citation

Chemical Properties

StorageStore at -20°C
M.Wt654.68
Cas No.210344-98-2
FormulaC30H43FN4O11
SynonymsBenzyloxycarbonyl-Ile-Glu(OMe)-Thr-Asp(OMe)-fluoromethylketone, Z-Ile-Glu(OMe)-Thr-Asp(OMe)-FMK
Solubility≥32.734mg/mL in DMSO
Chemical Namemethyl 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
SDFDownload SDF
Canonical SMILESCCC(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
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

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.

Biological Activity

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

Quality Control

Chemical structure

Z-IETD-FMK

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