BRD4770
Based on 5 publication(s) in Google Scholar
BRD4770 is a histone methyltransferase G9a inhibitor. BRD4770 reduces di- and trimethylation of lysine 9 on histone H3 (H3K9) with an EC50 of 5 μM, and has less or little effect toward H3K27me3, H3K36me3, H3K4me3, and H3K79me3. BRD4770 can activate the ataxia telangiectasia mutated (ATM) pathway and induce cell senescence.
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- Pureza: 99.79%
- No. CAS: 1374601-40-7
- Fòrmula: C25H23N3O3
- Peso molecular:413.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BRD4770
MoreVer todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
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EHMT2/G9a/KMT1C |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PANC-1 | IC50 |
5 μM
Compound: BRD4770
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Anticancer activity against human PANC1 cells
Anticancer activity against human PANC1 cells
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[PMID: 31276898] |
BRD4770 (0-20 μM; 72 hours; PANC-1 cells) treatment reduces the number of cells after 72 h[1].
BRD4770 (2.5-5 μM; 24 hours; PANC-1 cells) treatment decreases H3K9 trimethylation level by 23% in PANC-1 cells[1].
BRD4770 induces a senescent phenotype in a pancreatic cancer cell line. BRD4770 also inhibits both anchorage-dependent and -independent cell proliferation and induces G2/M cell-cycle arrest. BRD4770 activates the ataxia telangiectasia mutated (ATM) pathway without inducing DNA damage, while the ataxia telangiectasia and Rad3-related protein (ATR) pathway is not affected[1].
BRD4770 also induces increased levels of lysine acetylation in cells without inhibiting histone deacetylases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC-1 cells
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Concentration:0 µM, 0.625 µM, 1.25 µM, 2.5 µM, 5 µM, 10 µM, 20 µM
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Incubation Time:72 hours
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Result:Reduced the number of cells after 72 h.
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Cell Line:PANC-1 cells
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Concentration:2.5 µM, 5 µM
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Incubation Time:24 hours
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Result:Decreased H3K9 trimethylation level by 23% in PANC-1 cells.
Chemical Information
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No. CAS 1374601-40-7
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Appearance Solid
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Peso molecular 413.47
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Fòrmula C25H23N3O3
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Color White to off-white
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SMILES
O=C(C1=CC=C2C(N=C(NC(C3=CC=CC=C3)=O)N2CCCC4=CC=CC=C4)=C1)OC
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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 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Cell Death Discov
G9a deficiency activates TMEM27 to promote ferroptosis and enhances radiosensitivity in head and neck squamous cell carcinoma. [Abstract]2025 Nov 10;11(1):517. PMID: 41213903 -
J Invest Dermatol
DNA Damage Stress Control Is a Truncated Large T Antigen and Euchromatic Histone Lysine Methyltransferase 2-Dependent Central Feature of Merkel Cell Carcinoma. [Abstract]2024 Jun 20:S0022-202X(24)01860-8. PMID: 38908781 -
J Nutr Biochem
Maternal carbohydrate-programming enhances carbohydrate utilization in zebrafish offspring by histone H3K9 methylation. [Abstract]2025 Nov 11:149:110184. PMID: 41232653 -
Front Cell Dev Biol
EZH2/EHMT2 Histone Methyltransferases Inhibit the Transcription of DLX5 and Promote the Transformation of Myelodysplastic Syndrome to Acute Myeloid Leukemia. [Abstract]2021 Aug 2;9:619795. PMID: 34409024
Solvente y solubilidad
DMSO : 5 mg/mL (12.09 mM; ultrasonic and warming and heat to 60°C; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% Methylcellulose/saline water
Solubility: 6.25 mg/mL (15.12 mM); Suspended solution; Need ultrasonic
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 (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4186 mL | 12.0928 mL | 24.1856 mL | 60.4639 mL |
| 5 mM | 0.4837 mL | 2.4186 mL | 4.8371 mL | 12.0928 mL | |
| 10 mM | 0.2419 mL | 1.2093 mL | 2.4186 mL | 6.0464 mL |
BRD4770 Related Classifications
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