| Size | Price | Stock | Qty |
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| 2mg |
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| Targets |
Z-YVAD-FMK primarily targets caspase-1, an inflammatory caspase that mediates the processing of pro-inflammatory cytokines such as IL-1β and IL-18. It also inhibits caspase-4 and caspase-5. By irreversibly binding to the active site of caspase-1, the compound prevents the cleavage of pro-inflammatory cytokines, thereby modulating inflammatory responses. This makes Z-YVAD-FMK a valuable tool for studying inflammation and caspase-mediated signaling pathways.
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| ln Vitro |
Z-YVAD-FMK (100 μM; 24 hours) considerably reduces butyrate's ability to suppress the development of Caco-2 cells [1]. On HepG2 and BEL-7402 cells, Z-YVAD-FMK (20 μM; 1 hour before; 24 hours) divides III-10. On HepG2 cells, Z-VAD-FMK lowers fluorescence from 19.88% to 8.34%. while lowering BEL-7402 cells' cell fluorescence from 17.56% to 11.
In vitro, Z-YVAD-FMK functions as a cell-permeable, irreversible inhibitor of caspase-1 and caspase-4. It exhibits anti-inflammatory activity by blocking caspase-1-mediated processing of pro-inflammatory cytokines such as IL-1β. Z-YVAD-FMK (100 μM; 24 hours) significantly reduces caspase-1 activity induced by LPS+Aβ and suppresses cleaved IL-1β, cleaved IL-18, and Iba-1 protein expression. In Caco-2 cells, Z-YVAD-FMK (100 μM; 24 hours) significantly reduces the growth inhibition caused by butyrate. |
| ln Vivo |
In vivo, Z-YVAD-FMK has been shown to exert anti-tumor effects in various models. As a caspase-1 inhibitor, it modulates inflammatory responses and has potential therapeutic applications in inflammatory diseases and cancer. However, specific in vivo efficacy data, including dosing regimens and animal models, are not extensively detailed in the available literature. Further studies are needed to fully characterize its in vivo pharmacological profile. The compound is a research tool for studying inflammation and apoptosis.
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| Enzyme Assay |
Cell-free assays for Z-YVAD-FMK involve measuring its inhibitory activity against purified caspase-1 or caspase-4. Enzyme activity is monitored using fluorogenic peptide substrates that are cleaved by active caspases. Inhibition is assessed by incubating the caspase with varying concentrations of Z-YVAD-FMK and measuring residual activity. IC50 values are determined from dose-response curves. The compound's irreversible binding mechanism can be confirmed by pre-incubation and dilution experiments. Chemical purity and identity are confirmed by HPLC and mass spectrometry.
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| Cell Assay |
Cell viability assay [1]
Cell Types: Caco-2 cells Tested Concentrations: 0-100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of Caco-2 cell growth. 98%[4]. Apoptosis analysis [1] Cell Types: BEL-7402 and HepG2 Cell Tested Concentrations: 20 μM Incubation Duration: First 1 hour; 24 hrs (hours) Experimental Results: Induced cells to undergo caspase-dependent apoptosis. In vitro cellular assays for Z-YVAD-FMK typically involve treating cells with the compound at various concentrations (e.g., 100 μM) for defined periods (e.g., 24 hours). Caspase-1 activity in cell lysates is measured using fluorogenic substrates. IL-1β and IL-18 processing is assessed by western blotting. Cell viability is assessed using standard assays such as MTT. In Caco-2 cells, the compound's effect on butyrate-induced growth inhibition is evaluated. Dose-response and time-course experiments are performed to determine optimal conditions. |
| Animal Protocol |
In vivo animal studies for Z-YVAD-FMK are conducted in models of inflammation, cancer, and neurodegenerative disease. The compound is administered via various routes including intraperitoneal or intravenous injection. Inflammatory markers such as IL-1β and IL-18 are measured in serum and tissues. Tumor growth is monitored in cancer models. However, specific dosing regimens and experimental protocols are not extensively documented in the available literature. Standard protocols for evaluating caspase inhibitors would typically be employed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Z-YVAD-FMK include a molecular weight of 630.66 g/mol and molecular formula C31H39FN4O9. As a peptide, it has limited oral bioavailability and is typically administered parenterally. The compound is cell-permeable, enabling intracellular delivery. It is typically stored as a lyophilized powder and reconstituted in DMSO or appropriate buffers before use. Detailed ADME parameters are not extensively reported in the available literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of Z-YVAD-FMK has been characterized in preclinical studies. As a caspase inhibitor, potential toxicities may include effects on normal apoptosis and immune function. The compound is intended for research use only and not for therapeutic applications in humans. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
Z-YVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-1 and caspase-4. It exhibits anti-inflammatory activity by blocking IL-1β processing and anti-tumor effects. Z-YVAD-FMK (100 μM; 24 hours) reduces caspase-1 activity and suppresses cleaved IL-1β and IL-18 expression. It is a research tool for studying inflammation, apoptosis, and caspase signaling.
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| Molecular Formula |
C31H39N4O9F
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|---|---|
| Molecular Weight |
630.66116
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| Exact Mass |
630.27
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| CAS # |
210344-97-1
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| PubChem CID |
644196
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| Appearance |
White to off-white solid powder
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
18
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| Heavy Atom Count |
45
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| Complexity |
1010
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC([C@H](NC([C@@H](NC(OCC1=CC=CC=C1)=O)CC2=CC=C(O)C=C2)=O)C(N[C@H](C(N[C@H](C(CF)=O)CC(OC)=O)=O)C)=O)C
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| InChi Key |
MVPQJUFFTWWKBT-LBDWYMBGSA-N
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| InChi Code |
InChI=1S/C31H39FN4O9/c1-18(2)27(30(42)33-19(3)28(40)34-23(25(38)16-32)15-26(39)44-4)36-29(41)24(14-20-10-12-22(37)13-11-20)35-31(43)45-17-21-8-6-5-7-9-21/h5-13,18-19,23-24,27,37H,14-17H2,1-4H3,(H,33,42)(H,34,40)(H,35,43)(H,36,41)/t19-,23-,24-,27-/m0/s1
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| Chemical Name |
methyl (3S)-5-fluoro-3-[[(2S)-2-[[(2S)-2-[[(2S)-3-(4-hydroxyphenyl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-3-methylbutanoyl]amino]propanoyl]amino]-4-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 : ~125 mg/mL (~198.21 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.30 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 (3.30 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 (3.30 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 | 1.5856 mL | 7.9282 mL | 15.8564 mL | |
| 5 mM | 0.3171 mL | 1.5856 mL | 3.1713 mL | |
| 10 mM | 0.1586 mL | 0.7928 mL | 1.5856 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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