BRD3308
Based on 1 publication(s) in Google Scholar
BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
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- Pureté: 98.34%
- CAS No.: 1550053-02-5
- Formule: C15H14FN3O2
- Masse moléculaire:287.29
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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) BRD3308
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Customer Validation & Images
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WB
Activité biologique
Description
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HDAC3 54 nM (IC50) |
HDAC3 29 nM (Ki) |
HDAC1 1260 nM (IC50) |
HDAC1 5100 nM (Ki) |
HDAC2 1340 nM (IC50) |
HDAC2 6300 nM (Ki) |
HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Sf9 | IC50 |
1080 nM
Compound: 28; BRD3308
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Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
Inhibition of recombinant human full length C-terminal His/FALG-tagged HDAC1 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence
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[PMID: 30735902] |
| Sf9 | IC50 |
1150 nM
Compound: 28; BRD3308
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Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
Inhibition of recombinant human full length C-terminal FLAG-tagged HDAC2 expressed in Sf9 insect cells using FAM-labeled acetylated peptide A as substrate preincubated for 3 hrs followed by substrate addition and measured after 60 mins by fluorescence ass
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[PMID: 30735902] |
In Vitro
BRD3308 (5-30 μM; 6-24 hours) treatment increases HIV-1 expression in the 2D10 cell line[1].
BRD3308 (15 μM; overnight) is able to induce outgrowth of HIV-1 from latently infected cells ex vivo in resting CD4+ T cells[1]. BRD3308 inhibits HDAC1, HDAC2 and HDAC3 with Ki values of 5.1 μM, 6.3 μM and 29 nM, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:2D10 cells
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Concentration:5 µM, 10 µM, 15 µM, or 30 µM
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Incubation Time:6 hours, 12 hours, 18 hours, or 24 hours
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Result:An increase in HIV-1 expression was observed.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Zucker Diabetic Fatty (Obese) rats (6-week-old)[2]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection; every second day
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Result:Reduced hyperglycaemia and increased insulin secretion in a rat model of type 2 diabetes.
Chemical Information
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CAS No. 1550053-02-5
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Appearance Solid
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Masse moléculaire 287.29
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Formule C15H14FN3O2
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Color Off-white to light yellow
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SMILES
O=C(C)NC1=CC=C(C(NC2=CC=C(F)C=C2N)=O)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 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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Cell Rep Med
Epigenetic profiling identifies markers of endocrine resistance and therapeutic options for metastatic castration-resistant prostate cancer. [Abstract]2025 Jul 15;6(7):102215. PMID: 40609538
BRD3308 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Jul 15;6(7):102215. [Abstract]
Western blot of HDAC3, H3K27ac and control protein HSP90 for 3 HDAC inhibitors, vorinstat (pan-HDACi), BRD3308 (1, 10 μM) (specific-HDAC3i) and RFGP966 (specific HDAC3i) for cPDX LuCaP 189.4 (Top) and cPDX LuCaP 35 (Bottom).
Solvant et solubilité
In Vitro:
DMSO : 250 mg/mL (870.20 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)
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: ≥ 2.08 mg/mL (7.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
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 (275 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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Instruction de manipulation (2659 KB)
Références
[1]. Barton KM, et al. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684. [Content Brief]
[2]. Lundh M, et al. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7. [Content Brief]
[3]. Wagner FF, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016 Feb 19;11(2):363-74. [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 |
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| DMSO | 1 mM | 3.4808 mL | 17.4040 mL | 34.8080 mL | 87.0201 mL |
| 5 mM | 0.6962 mL | 3.4808 mL | 6.9616 mL | 17.4040 mL | |
| 10 mM | 0.3481 mL | 1.7404 mL | 3.4808 mL | 8.7020 mL | |
| 15 mM | 0.2321 mL | 1.1603 mL | 2.3205 mL | 5.8013 mL | |
| 20 mM | 0.1740 mL | 0.8702 mL | 1.7404 mL | 4.3510 mL | |
| 25 mM | 0.1392 mL | 0.6962 mL | 1.3923 mL | 3.4808 mL | |
| 30 mM | 0.1160 mL | 0.5801 mL | 1.1603 mL | 2.9007 mL | |
| 40 mM | 0.0870 mL | 0.4351 mL | 0.8702 mL | 2.1755 mL | |
| 50 mM | 0.0696 mL | 0.3481 mL | 0.6962 mL | 1.7404 mL | |
| 60 mM | 0.0580 mL | 0.2901 mL | 0.5801 mL | 1.4503 mL | |
| 80 mM | 0.0435 mL | 0.2176 mL | 0.4351 mL | 1.0878 mL | |
| 100 mM | 0.0348 mL | 0.1740 mL | 0.3481 mL | 0.8702 mL |
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