MX1013
Based on 1 publication(s) in Google Scholar
MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM.
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- Pureté: 95.04%
- CAS No.: 582316-00-5
- Formule: C18H23FN2O6
- Masse moléculaire:382.38
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MX1013
MoreVoir tous les produits spécifiques à Isoform Caspase
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Activité biologique
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Caspase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | EC50 |
>100 μM
Compound: 7
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Inhibitory activity against SARS coronavirus FFMI replication in Caco-2 cells
Inhibitory activity against SARS coronavirus FFMI replication in Caco-2 cells
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[PMID: 16451084] |
| Vero | CC50 |
>100 μM
Compound: 7
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Cytotoxicity against Vero (CCL81) cells
Cytotoxicity against Vero (CCL81) cells
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[PMID: 16451084] |
MX1013 inhibits caspases 1, 3, 6, 7, 8, and 9, with IC50 values ranging from 5 to 20 nm. MX1013 is selective for caspases, and is a poor inhibitor of noncaspase proteases, such as cathepsin B, calpain I, or Factor Xa (IC50 values >10 μm)[1].
MX1013 inhibits three key markers of apoptosis: the proteolytic maturation of caspase 3, the caspase-mediated cleavage of PARP, and the fragmentation of genomic DNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T-lymphocytes
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Concentration:0, 0.05, 0.1, 0.25, 0.5 μM
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Incubation Time:Preincubated for 2 h
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Result:Neither caspase 3 processing nor PARP cleavage could be detected at 0.5 μM. At concentrations of 0.05 μM, caspase 3 processing and PARP cleavage were still markedly reduced.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female ND4 Swiss Webster mice (16.5-21 g)[1]
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Dosage:0, 0.25, 1, 10 mg/kg (formulated in an aqueous vehicle containing 50 mm Tris-HCl, pH 8.0)
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Administration:Injected i.v.
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Result:The lowest dose of 0.25 mg/kg protected 66% of the mice from the lethal effects of anti-Fas antibody at the 3 h time point, and 1 and 10 mg/kg dose protected 100% of the mice at the 3 h time point.
Chemical Information
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CAS No. 582316-00-5
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Appearance Solid
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Masse moléculaire 382.38
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Formule C18H23FN2O6
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Color White to off-white
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SMILES
O=C(O)CC(NC([C@@H](NC(OCC1=CC=CC=C1)=O)C(C)C)=O)C(CF)=O
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Synonyms
CV1013; Z-VD-FMK
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Infect Dis
Role of Histiocyte-Derived frHMGB1 as a Facilitator in Non-Canonical Pyroptosis of Monocytes/Macrophages in Lethal Sepsis. [Abstract]2024 Aug 16;230(2):298-308. PMID: 38243905
Solvant et solubilité
DMSO : 100 mg/mL (261.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.54 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6152 mL | 13.0760 mL | 26.1520 mL | 65.3800 mL |
| 5 mM | 0.5230 mL | 2.6152 mL | 5.2304 mL | 13.0760 mL | |
| 10 mM | 0.2615 mL | 1.3076 mL | 2.6152 mL | 6.5380 mL | |
| 15 mM | 0.1743 mL | 0.8717 mL | 1.7435 mL | 4.3587 mL | |
| 20 mM | 0.1308 mL | 0.6538 mL | 1.3076 mL | 3.2690 mL | |
| 25 mM | 0.1046 mL | 0.5230 mL | 1.0461 mL | 2.6152 mL | |
| 30 mM | 0.0872 mL | 0.4359 mL | 0.8717 mL | 2.1793 mL | |
| 40 mM | 0.0654 mL | 0.3269 mL | 0.6538 mL | 1.6345 mL | |
| 50 mM | 0.0523 mL | 0.2615 mL | 0.5230 mL | 1.3076 mL | |
| 60 mM | 0.0436 mL | 0.2179 mL | 0.4359 mL | 1.0897 mL | |
| 80 mM | 0.0327 mL | 0.1634 mL | 0.3269 mL | 0.8172 mL | |
| 100 mM | 0.0262 mL | 0.1308 mL | 0.2615 mL | 0.6538 mL |
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