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Z-WEHD-FMK is a novel, highly potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis.
| ln Vitro |
Nearly entirely blocks C is Z-WEHD-FMK (80 μM; 9 hours). golgin-84 cleavage brought on by trachomatis and raises GM130 expression in cells [1]. Z-WEHD-FMK successfully inhibited 0909I E. 30 minutes before to exposure to E. piscicida. pyroptosis morphology and piscicida-induced cytotoxicity in ZF4 cells. Moreover, it prevents cytotoxicity brought on by the administration of cytosolic LPS [2]. Significantly, Z-WEHD-FMK (20 μM; 18–24 hours after Cr3+, Ni2+, and Co2+) elicited a 76%–86% reduction in IL-1β production, with a similar reduction observed at 200–400 ppm Cr3+ 35%. Inhibitors of caspase-1 caused a reduction of 40% to 45% when Ni2+ concentrations were 48 ppm or higher. Ultimately, the caspase-1 inhibitor reduced the levels of Co2+ to below the detection threshold at 6 ppm, and in bone marrow-derived macrophages (BMDM) at 12 to 24 ppm, the reduction might range from 40% to 48%[3].
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Chlamydia trachomatis-infected or mock-infected HeLa cells Tested Concentrations: 80 μM Incubation Duration: 9 hrs (hours) Experimental Results: Increased expression of golgin-84 and GM130. Cell viability assay [2] Cell Types: Mycoplasma-free ZF4 cells Tested Concentrations: Incubation Duration: 30 minutes before exposure to E. piscicida Experimental Results: Inhibition of cytotoxicity and pyroptosis morphology of ZF4 cells. |
| References |
| Molecular Formula |
C37H42N7O10F
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|---|---|
| Molecular Weight |
763.76868
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| Exact Mass |
763.298
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| CAS # |
210345-00-9
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| PubChem CID |
25108687
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.205
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
23
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| Heavy Atom Count |
55
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| Complexity |
1330
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| Defined Atom Stereocenter Count |
4
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| SMILES |
COC(=O)CC[C@@H](C(=O)N[C@@H](CC1=CN=CN1)C(=O)N[C@@H](CC(=O)OC)C(=O)CF)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)NC(=O)OCC4=CC=CC=C4
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| InChi Key |
NLZNSSWGRVBWIX-KRCBVYEFSA-N
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| InChi Code |
InChI=1S/C37H42FN7O10/c1-53-32(47)13-12-27(34(49)44-30(15-24-19-39-21-41-24)36(51)43-28(31(46)17-38)16-33(48)54-2)42-35(50)29(14-23-18-40-26-11-7-6-10-25(23)26)45-37(52)55-20-22-8-4-3-5-9-22/h3-11,18-19,21,27-30,40H,12-17,20H2,1-2H3,(H,39,41)(H,42,50)(H,43,51)(H,44,49)(H,45,52)/t27-,28-,29-,30-/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-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoate
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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. |
| 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) |
DMSO : ~100 mg/mL (~130.93 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.27 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 25.0 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: ≥ 2.5 mg/mL (3.27 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 25.0 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: ≥ 2.5 mg/mL (3.27 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 | 1.3093 mL | 6.5465 mL | 13.0929 mL | |
| 5 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL | |
| 10 mM | 0.1309 mL | 0.6546 mL | 1.3093 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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