Ac-DMLD-CMK TFA
Based on 1 Customer Validation
Ac-DMLD-CMK TFA is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DMLD-CMK TFA binds directly to the catalytic domain of caspase-3, blocks caspase-3-mediated cleavage of GSDME, inhibits the activation of caspase 3 and Gsdme in the caspase 3-Gsdme signaling pathway, and reduces the levels of pyroptosis and apoptosis as well as the expression of LDH, IL-6, IL-1β and IL-18. Ac-DMLD-CMK TFA alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity.
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- Pureté : 98.44%
- Formule: C24H36ClF3N4O11S
- Masse moléculaire:681.08
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
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Activité biologique
Description
IC50 & Target
[1]|
Caspase 3 |
In Vitro
Ac-DMLD-CMK TFA (5 μM; 6 h pre-incubation) inhibits simvastatin-induced pyroptosis and cell viability reduction in MGC-803 human gastric cancer cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ac-DMLD-CMK TFA (5 mg/kg; i.p.; single dose 3 h pre-CLP) significantly reduces CLP-induced acute lung injury in male C57BL/6 J mice by inhibiting caspase-3/GSDME-mediated pyroptosis and apoptosis, as evidenced by reduced lung injury scores, inflammatory mediator levels, and cell death markers[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 6-8 weeks old, 20-25 g, cisplatin-induced)[1]
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Dosage:5 mg/kg/day
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Administration:i.p.; single injection 1 hour prior to cisplatin administration
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Result:Reduced serum creatinine and blood urea nitrogen levels compared to cisplatin-only treated mice.
Alleviated renal tubular epithelial cell death.
Reduced levels of cleaved mouse Gsdme (Gsdme-N) and cleaved caspase 3, with no significant effect on full-length mouse Gsdme (Gsdme-FL).
Suppressed renal mRNA expression of Ngal, Il6,Tnfa, and Il1b; did not affect Kim1 expression.
Chemical Information
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Appearance Solid
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Masse moléculaire 681.08
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Formule C24H36ClF3N4O11S
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Color White to off-white
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Sequence
Ac-Asp-Met-Leu-{Asp-CMK}
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Sequence Shortening
Ac-DML-{Asp-CMK}
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (146.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
In Vivo:
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 (3.67 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 (3.67 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 (278 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
[1]. Shen X, et al. Caspase 3/GSDME-dependent pyroptosis contributes to chemotherapy drug-induced nephrotoxicity. Cell Death Dis. 2021;12(2):186. Published 2021 Feb 15. [Content Brief]
[2]. Qin H, et al. Inhibiting caspase-3/GSDME-mediated pyroptosis ameliorates septic lung injury in mice model. Mol Immunol. 2024;172:96-104. [Content Brief]
[3]. Xia Y, et al. Antitumor Effect of Simvastatin in Combination With DNA Methyltransferase Inhibitor on Gastric Cancer via GSDME-Mediated Pyroptosis. Front Pharmacol. 2022;13:860546. Published 2022 Apr 20. [Content Brief]
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 (sealed storage, away from moisture). 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 | 1.4683 mL | 7.3413 mL | 14.6826 mL | 36.7064 mL |
| 5 mM | 0.2937 mL | 1.4683 mL | 2.9365 mL | 7.3413 mL | |
| 10 mM | 0.1468 mL | 0.7341 mL | 1.4683 mL | 3.6706 mL | |
| 15 mM | 0.0979 mL | 0.4894 mL | 0.9788 mL | 2.4471 mL | |
| 20 mM | 0.0734 mL | 0.3671 mL | 0.7341 mL | 1.8353 mL | |
| 25 mM | 0.0587 mL | 0.2937 mL | 0.5873 mL | 1.4683 mL | |
| 30 mM | 0.0489 mL | 0.2447 mL | 0.4894 mL | 1.2235 mL | |
| 40 mM | 0.0367 mL | 0.1835 mL | 0.3671 mL | 0.9177 mL | |
| 50 mM | 0.0294 mL | 0.1468 mL | 0.2937 mL | 0.7341 mL | |
| 60 mM | 0.0245 mL | 0.1224 mL | 0.2447 mL | 0.6118 mL | |
| 80 mM | 0.0184 mL | 0.0918 mL | 0.1835 mL | 0.4588 mL | |
| 100 mM | 0.0147 mL | 0.0734 mL | 0.1468 mL | 0.3671 mL |
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