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| 2mg |
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| 10mg |
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| 25mg |
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Purity: ≥98%
Z-DEVD-FMK, a tetrapeptide compound, is a novel, potent, specific, cell-permeable and irreversible caspase-3 inhibitor with IC50 of 18 μM. Compared to caspase-6, caspase-7, and caspase-10, it is relatively more selective for caspase-3.
| Targets |
Caspase-3 (IC50 = 18 μM)
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| ln Vitro |
Z-DEVD-FMK (1–200 μM) inhibits D4-GDI cleavage and apoptosis in a concentration-dependent manner. [1] Z-DEVD-FMK significantly inhibits the activation of caspase 3 and lessens ceramide-induced cardiomyocyte death. [3] In cultured brain microvessel endothelial cells, Z-DEVD-FMK (100 μM) inhibits OxyHb's effects on DNA ladders, caspase-2 and -3 activity, cell detachment, and PARP cleavage. [4] Caspase-3 activity increases brought on by MPP+ are prevented by Z-DEVD-FMK (100 μM). With an IC50 of 18 μM, Z-DEVD-FMK inhibits 6-OHDA-induced apoptotic cell death in a dose-dependent manner. [5]
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| ln Vivo |
Z-DEVD-FMK significantly improves neurological recovery both before and after injury by significantly reducing post-traumatic apoptosis. [2]
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| Enzyme Assay |
Utilizing fluorescent-based substrate, the activities of caspase-3 and caspase-9 are measured. Following treatment, the cells are resuspended in 10 mM digitonin-containing lysis buffer (50 mM Tris HCl, 1 mM EDTA, and 10 mM EGTA) for 20 min at 37°C. Ac-DEVD-AFC for caspase-3 or Ac-LEHD-AFC for caspase-9 are applied to supernatants for 1 hour at 37 degrees Celsius. Fluorescence is then measured using a Gemini XS fluorescence plate reader at excitation at 400 nm and emission at 505 nm.
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| Cell Assay |
Using the widely used MTT assay (3-(4,5-dimethylthiazol-3-yl)-2,5-diphenyl tetrazolium bromide), cell death in N27 cells is assessed after incubation 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. The cells are then treated and incubated for 3 hours at 37 degrees Celsius in serum-free medium containing 0.25 mg/ml MTT. Using a SpectraMax microplate reader and a reference wavelength of 630 nm, the formation of formazan from tetrazolium is measured at 570 nm.
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| Animal Protocol |
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| References | |||
| Additional Infomation |
Z-DEVD-FMK is a tetrapeptide consisting of Fmoc-L-aspartic acid 4-methyl ester, methyl L-alpha-glutamic acid 5-methyl ester, L-valine and the fluoromethyl ketone derived from the 1-carboxy group of L-aspartic acid 4-methyl ester coupled in sequence. It is a specific, irreversible caspase-3 inhibitor that also shows potent inhibition of caspase-6, caspase-7, caspase-8, and caspase-10. It has a role as an apoptosis inhibitor, an EC 3.4.22.56 (caspase-3) inhibitor and a neuroprotective agent.
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| Molecular Formula |
C30H41FN4O12
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| Molecular Weight |
668.66
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| Exact Mass |
668.27
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| Elemental Analysis |
C, 53.89; H, 6.18; F, 2.84; N, 8.38; O, 28.71
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| CAS # |
210344-95-9
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| Related CAS # |
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| PubChem CID |
16760394
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
914.2±65.0 °C at 760 mmHg
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| Flash Point |
506.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.512
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
47
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| Complexity |
1110
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| Defined Atom Stereocenter Count |
4
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| SMILES |
O=C(N[C@@H](C(C)C)C(N[C@H](C(CF)=O)CC(OC)=O)=O)[C@H](CCC(OC)=O)NC([C@H](CC(OC)=O)NC(OCC1=CC=CC=C1)=O)=O
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| InChi Key |
GBJVAVGBSGRRKN-JYEBCORGSA-N
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| InChi Code |
InChI=1S/C30H41FN4O12/c1-17(2)26(29(42)33-20(22(36)15-31)13-24(38)45-4)35-27(40)19(11-12-23(37)44-3)32-28(41)21(14-25(39)46-5)34-30(43)47-16-18-9-7-6-8-10-18/h6-10,17,19-21,26H,11-16H2,1-5H3,(H,32,41)(H,33,42)(H,34,43)(H,35,40)/t19-,20-,21-,26-/m0/s1
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| Chemical Name |
methyl (4S)-5-[[(2S)-1-[[(3S)-5-fluoro-1-methoxy-1,4-dioxopentan-3-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-4-[[(2S)-4-methoxy-4-oxo-2-(phenylmethoxycarbonylamino)butanoyl]amino]-5-oxopentanoate
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| Synonyms |
ZDEVDfmk; Z-DEVD-fmk; Z DEVD fmk
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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 |
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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: ≥ 1 mg/mL (1.50 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.50 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 2% DMSO+30% PEG 400+5% Tween 80+ddH2O: 1mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4955 mL | 7.4776 mL | 14.9553 mL | |
| 5 mM | 0.2991 mL | 1.4955 mL | 2.9911 mL | |
| 10 mM | 0.1496 mL | 0.7478 mL | 1.4955 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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