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Purity: ≥98%
Z-IETD-FMK, also known as Z-IE(OMe)TD(OMe)-FMK, is a novel Caspase-8/9 inhibitor that is specific, selective, irreversible, and cell permeable. Z-IETD-FMK works by preventing PHA- or anti-CD3 plus anti-CD28-induced T cell proliferation without harming dormant T cells. Normal cell growth is unaffected by Z-IETD-FMK in the absence of an activation signal. When present in concentrations of 100μM, Z-IETD-FMK has also been discovered to significantly inhibit NF-κB activation. In addition to its capacity to suppress cell proliferation, Z-IETD-FMK is also said to suppress TRAIL-mediated cell apoptosis. In both HCT116 and SW480 cells, it equally protects procaspases 9, 2, and 3 as well as PARP.
| Targets |
Caspase-8
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|---|---|
| ln Vitro |
In retinal cells exposed to various apoptotic stimuli, Z-IETD-FMK, which blocks caspase-8 cleavage and only partially blocks caspase-3 and PARP cleavage, inhibits the execution of apoptosis.[1]
Z-IETD-FMK (50 μM) significantly inhibits the activation of caspase 3 and lessens the death of cardiomyocytes brought on by ceramide.[2] The production of activated/memory T cells, T cell cytokines, and NF-kappaB responses to TCR:CD3 engagement in T cell cultures are all impacted by Z-IETD-FMK'scaspase-8inhibition.[3] |
| ln Vivo |
Z-IETD-FMK inhibits caspase-8 in living organisms, which decreases memory/activated CD4 and CD8 T cells and raises susceptibility to T. cruzi infection.[3]
Injured retinal ganglion cells are encouraged to regenerate and survive after CNS injuries by Z-IETD-FMK. [4] |
| Cell Assay |
Drugs and ceramide were simultaneously added to the cell culture medium, and after 24 hours, the number of living cells was counted.
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| Animal Protocol |
T. cruzi-infected mice
0.4 mg/3 days |
| References |
| Molecular Formula |
C30H43FN4O11
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|---|---|---|
| Molecular Weight |
654.68
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| Exact Mass |
654.291
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| Elemental Analysis |
C, 53.67; H, 6.27; F, 3.03; N, 8.94; O, 28.08
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| CAS # |
210344-98-2
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| Related CAS # |
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| PubChem CID |
25108681
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| Appearance |
White to light yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
925.7±65.0 °C at 760 mmHg
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| Flash Point |
513.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.518
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| LogP |
3.92
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
46
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| Complexity |
1050
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| Defined Atom Stereocenter Count |
6
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| SMILES |
FC([H])([H])C([C@@]([H])(C([H])([H])C(=O)OC([H])([H])[H])N([H])C([C@]([H])([C@@]([H])(C([H])([H])[H])O[H])N([H])C([C@@]([H])(C([H])([H])C([H])([H])C(=O)OC([H])([H])[H])N([H])C([C@@]([H])([C@@]([H])(C([H])([H])[H])C([H])([H])C([H])([H])[H])N([H])C(=O)OC([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O)=O)=O)=O
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| InChi Key |
PHLCQASLWHYEMX-DEKIMQJDSA-N
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| InChi Code |
InChI=1S/C30H43FN4O11/c1-6-17(2)25(35-30(43)46-16-19-10-8-7-9-11-19)28(41)32-20(12-13-23(38)44-4)27(40)34-26(18(3)36)29(42)33-21(22(37)15-31)14-24(39)45-5/h7-11,17-18,20-21,25-26,36H,6,12-16H2,1-5H3,(H,32,41)(H,33,42)(H,34,40)
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| Chemical Name |
methyl (4S)-5-[[(2S,3R)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-4-[[(2S,3S)-3-methyl-2-(phenylmethoxycarbonylamino)pentanoyl]amino]-5-oxopentanoate
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| Synonyms |
Z-IE(OMe)TD(OMe)-FMK; Z-IETD-FMK; Granzyme B Inhibitor III; MDK-4982; MDK4982; MDK 4982; Z-Ile-Glu(OMe)-Thr-Asp(OMe)-CH₂F
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.18 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.18 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.18 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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