ML604440
Based on 3 publication(s) in Google Scholar
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.28%
- No. CAS: 1140517-08-3
- Fòrmula: C17H24BF3N2O4
- Peso molecular:388.19
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) ML604440
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Actividad biológica
proteasome β1i (LMP2) subunit inhibitor[1]
ML604440 (300 nM; overnight) treatment shows no influence on the surface expression of H-2Kb in wt or LMP7-deficient mice splenocytes[2].
ML604440 (300 nM; 24 h) treatment shows no significant inhibition of IL-6 secretion by mouse splenocytes or human PBMCs[2].
ML604440 (300 nM; 3 d) shows no influence on the percentage of IL-17A-producing CD4+ T cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (6-8-wks old) injected with anti-platelet monoclonal antibody[3]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 10 mg/kg; once daily; 7 days
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Result:Inhibited LMP2 in vivo.
Showed no significant improvement in platelet counts in mice immunized by monoclonal rat anti-mouse CD41 platelet antibody.
Chemical Information
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No. CAS 1140517-08-3
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Appearance Solid
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Peso molecular 388.19
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Fòrmula C17H24BF3N2O4
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Color White to yellow
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SMILES
CC(C)C[C@@H](B(O)O)NC(C(NC(C1=CC=CC=C1C(F)(F)F)=O)(C)C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Redox Biol
Deficient immunoproteasome assembly drives gain of α-synuclein pathology in Parkinson's disease. [Abstract]2021 Nov:47:102167. PMID: 34662812 -
Cell Death Dis
Inhibition of p38 MAPK or immunoproteasome overcomes resistance of chronic lymphocytic leukemia cells to Bcl-2 antagonist venetoclax. [Abstract]2022 Oct 8;13(10):860. PMID: 36209148 -
J Med Chem
α-Aminoboronic Acid Moieties in Boro Dipeptides Modulate Proteasome Subunit Selectivity and Provide Access to Compounds with Potent Anticancer and Anti-Inflammatory Activity. [Abstract]2025 Dec 25;68(24):26405-26417. PMID: 41344819
Solvente y solubilidad
DMSO : 100 mg/mL (257.61 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 (6.44 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 (6.44 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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. de Bruin G, et al. Structure-based design of β1i or β5i specific inhibitors of human immunoproteasomes. J Med Chem. 2014 Jul 24;57(14):6197-209 [Content Brief]
[2]. Basler M, et al. Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity. EMBO Rep. 2018 Dec;19(12). pii: e46512. [Content Brief]
[3]. Sheng-Hong Du, et al. Co-Inhibition of the Immunoproteasome Subunits LMP2 and LMP7 Ameliorates Immune Thrombocytopenia. Front Immunol. 2021 Jan 20;11:603278. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5761 mL | 12.8803 mL | 25.7606 mL | 64.4015 mL |
| 5 mM | 0.5152 mL | 2.5761 mL | 5.1521 mL | 12.8803 mL | |
| 10 mM | 0.2576 mL | 1.2880 mL | 2.5761 mL | 6.4401 mL | |
| 15 mM | 0.1717 mL | 0.8587 mL | 1.7174 mL | 4.2934 mL | |
| 20 mM | 0.1288 mL | 0.6440 mL | 1.2880 mL | 3.2201 mL | |
| 25 mM | 0.1030 mL | 0.5152 mL | 1.0304 mL | 2.5761 mL | |
| 30 mM | 0.0859 mL | 0.4293 mL | 0.8587 mL | 2.1467 mL | |
| 40 mM | 0.0644 mL | 0.3220 mL | 0.6440 mL | 1.6100 mL | |
| 50 mM | 0.0515 mL | 0.2576 mL | 0.5152 mL | 1.2880 mL | |
| 60 mM | 0.0429 mL | 0.2147 mL | 0.4293 mL | 1.0734 mL | |
| 80 mM | 0.0322 mL | 0.1610 mL | 0.3220 mL | 0.8050 mL | |
| 100 mM | 0.0258 mL | 0.1288 mL | 0.2576 mL | 0.6440 mL |
ML604440 Related Classifications
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