MS417
Based on 4 publication(s) in Google Scholar
MS417 is a selective BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with weak selectivity at CBP BRD (IC50, 32.7 μM).
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- Pureté: 99.79%
- CAS No.: 916489-36-6
- Formule: C20H19ClN4O2S
- Masse moléculaire:414.91
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Stockage:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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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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Publications Citing Use of MedChemExpress (MCE) MS417
More
Activité biologique
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BET |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | IC50 |
0.038 μM
Compound: 6h
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Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay
Immunosuppressive activity in BALB/c mouse splenic T cells assessed as inhibition of PMA/CD28 induced cell proliferation after 24 hrs by [methyl-3H]thymidine incorporation assay
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[PMID: 26869194] |
MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM and Kds of 36.1, 25.4 nM, respectively, with less selectivity at CBP BrD (IC50, 32.7 μM). MS417 effectively blocks BRD4 binding to NF-κB, almost completely suppresses TNFα-induced NF-κB transcription activation in human embryonic kidney 293T cells at 1 μM and also reduces NF-κB p65 acetylation in the HIV-infected RTECs. MS417 (1 μM) modulation of gene transcription in HIV-infected human primary renal tubular epithelial cells. In addition, MS417 suppresses NF-κB-targeted cytokines and chemokines[1].
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.
Chemical Information
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CAS No. 916489-36-6
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Appearance Solid
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Masse moléculaire 414.91
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Formule C20H19ClN4O2S
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Color Light yellow to yellow
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SMILES
O=C(OC)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1
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Synonyms
GTPL7512
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
2022 May 31;13(1):3016. PMID: 35641523 -
Curr Biol
A small proportion of X-linked genes contribute to X chromosome upregulation in early embryos via BRD4-mediated transcriptional activation. [Abstract]2022 Oct 24;32(20):4397-4410.e5. PMID: 36108637 -
Cell Mol Life Sci
Targeting BRD4 mitigates hepatocellular lipotoxicity by suppressing the NLRP3 inflammasome activation and GSDMD-mediated hepatocyte pyroptosis. [Abstract]2024 Jul 9;81(1):295. PMID: 38977508 -
Stem Cell Rev Rep
Disruption of CTCF Boundary at HOXA Locus Promote BET Inhibitors' Therapeutic Sensitivity in Acute Myeloid Leukemia. [Abstract]2020 Dec;16(6):1280-1291. PMID: 33057942
Solvant et solubilité
Ethanol : 50 mg/mL (120.51 mM; Need ultrasonic)
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 (stored under nitrogen). 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 (stored under nitrogen). 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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.03 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 EtOH 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.03 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 EtOH 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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
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.
Working solution concentration: 0.22 mg/mL
Pureté et documentation
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Fiche technique (281 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 (stored under nitrogen). 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 |
|---|---|---|---|---|---|
| Ethanol | 1 mM | 2.4102 mL | 12.0508 mL | 24.1016 mL | 60.2540 mL |
| 5 mM | 0.4820 mL | 2.4102 mL | 4.8203 mL | 12.0508 mL | |
| 10 mM | 0.2410 mL | 1.2051 mL | 2.4102 mL | 6.0254 mL | |
| 15 mM | 0.1607 mL | 0.8034 mL | 1.6068 mL | 4.0169 mL | |
| 20 mM | 0.1205 mL | 0.6025 mL | 1.2051 mL | 3.0127 mL | |
| 25 mM | 0.0964 mL | 0.4820 mL | 0.9641 mL | 2.4102 mL | |
| 30 mM | 0.0803 mL | 0.4017 mL | 0.8034 mL | 2.0085 mL | |
| 40 mM | 0.0603 mL | 0.3013 mL | 0.6025 mL | 1.5064 mL | |
| 50 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2051 mL | |
| 60 mM | 0.0402 mL | 0.2008 mL | 0.4017 mL | 1.0042 mL | |
| 80 mM | 0.0301 mL | 0.1506 mL | 0.3013 mL | 0.7532 mL | |
| 100 mM | 0.0241 mL | 0.1205 mL | 0.2410 mL | 0.6025 mL |
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