BRD-6929
Based on 3 publication(s) in Google Scholar
BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.01%
- No. CAS: 849234-64-6
- Fòrmula: C19H17N3O2S
- Peso molecular:351.42
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) BRD-6929
More
Actividad biológica
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HDAC1 1 nM (IC50) |
HDAC2 8 nM (IC50) |
HDAC3 458 nM (IC50) |
HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Epithelial cell | IC50 |
>50 μM
Compound: 19
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Cytotoxicity against human mammary epithelial cells by MTT assay
Cytotoxicity against human mammary epithelial cells by MTT assay
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[PMID: 17941625] |
| HCT-116 | GI50 |
0.11 μM
Compound: 60
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Antiproliferative activity against human HCT116 cells assessed as cell viability
Antiproliferative activity against human HCT116 cells assessed as cell viability
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[PMID: 18182289] |
| HCT-116 | IC50 |
0.5 μM
Compound: 19
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Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
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[PMID: 17941625] |
| Jurkat | CC50 |
12.6 μM
Compound: 1; TPB
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Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human Jurkat cells assessed as reduction in cell viability after 72 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 29541372] |
| Jurkat | IC50 |
204 nM
Compound: 1
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Inhibition of FLAG-tagged HDAC1 S113A mutant (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
Inhibition of FLAG-tagged HDAC1 S113A mutant (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
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[PMID: 24405391] |
| Jurkat | IC50 |
40 nM
Compound: 1
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Inhibition of wild-type FLAG-tagged HDAC1 (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
Inhibition of wild-type FLAG-tagged HDAC1 (unknown origin) expressed in Jurkat cells after 2 hrs by Fluor de lys staining-based fluorimetric analysis
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[PMID: 24405391] |
| KB | IC50 |
5.27 μM
Compound: SHI1:2
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Cytotoxicity against human KB cells after 72 hrs by MTS assay
Cytotoxicity against human KB cells after 72 hrs by MTS assay
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[PMID: 25899338] |
| Sf9 | IC50 |
0.001 μM
Compound: 60
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Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate
Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate
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[PMID: 27377864] |
| Sf9 | IC50 |
0.013 μM
Compound: 60
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Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate preincubated for 3 hrs measured after 60 mins by flu
Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate preincubated for 3 hrs measured after 60 mins by flu
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[PMID: 27377864] |
| U-937 | CC50 |
14 μM
Compound: 1; TPB
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Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
Cytotoxicity against human U937 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Glo luminescent cell viability assay
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[PMID: 29541372] |
In vitro IC50 for HDAC1-9 by BRD-6929 using recombinant human HDAC enzymes and HDAC class-specific substrates. BRD-6929 and substrate are incubated for 180 min (HDAC1-3) to control for HDAC1-3 inhibition, BRD-6929 is against HDAC1, HDAC2, HDAC3 and HDAC4-9 with IC50s of 0.001 μM, 0.008 μM, 0.458 μM and >30 μM, respectively[1]. In vitro binding affinity (Ki) and kinetics (half-life ‘T1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 μM), the Ki values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T1/2 values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively[1]. BRD-6929 (1 and 10 uM) does not cause an increase or decrease in overall cell number in brain region specific primary cultures. Additionally, BRD-6929 (10 uM) causes an increase in H4K12 acetylation in brain region specific primary cultures (striatum)[1].BRD-6929 (1-10 uM; 6 hours) causes a significant increase in H2B acetylation in primary neuronal cell cultures. BRD-6929 (1-20 uM; 24 hours) induces a dose-dependent acetylation of H4K12ac with an EC50 of 7.2 μM in cultured neurons[1].BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1[3].
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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No. CAS 849234-64-6
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Appearance Solid
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Peso molecular 351.42
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Fòrmula C19H17N3O2S
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Color Off-white to gray
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SMILES
O=C(NC1=CC(C2=CC=CS2)=CC=C1N)C3=CC=C(NC(C)=O)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 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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Adv Sci (Weinh)
The Probiotic Parabacteroides johnsonii Ameliorates Metabolic Disorders Through Promoting BCAAs to BSCFAs Conversion. [Abstract]2025 Aug 7:e02624. PMID: 40772426 -
Clin Transl Med
2026 Feb;16(2):e70603. PMID: 41603084 -
bioRxiv
Butyrate rescues chlorpyrifos-induced social deficits through inhibition of class I histone deacetylases. [Abstract]2025 Oct 20:2025.10.19.683261. PMID: 41280077
Solvente y solubilidad
DMSO : 25 mg/mL (71.14 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.92 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 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]. Li-Huei Tsai, et al. Inhibition of hdac2 to promote memory. patent/US20120101147
[2]. Schroeder FA, et al. A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and altersmouse behavior in two mood-related tests. PLoS One. 2013 Aug 14;8(8):e71323. [Content Brief]
[3]. Huang L, et al. Elimination of HIV-1 Latently Infected Cells by Gnidimacrin and a Selective HDAC Inhibitor. ACS Med Chem Lett. 2018 Feb 6;9(3):268-273. [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 | 2.8456 mL | 14.2280 mL | 28.4560 mL | 71.1399 mL |
| 5 mM | 0.5691 mL | 2.8456 mL | 5.6912 mL | 14.2280 mL | |
| 10 mM | 0.2846 mL | 1.4228 mL | 2.8456 mL | 7.1140 mL | |
| 15 mM | 0.1897 mL | 0.9485 mL | 1.8971 mL | 4.7427 mL | |
| 20 mM | 0.1423 mL | 0.7114 mL | 1.4228 mL | 3.5570 mL | |
| 25 mM | 0.1138 mL | 0.5691 mL | 1.1382 mL | 2.8456 mL | |
| 30 mM | 0.0949 mL | 0.4743 mL | 0.9485 mL | 2.3713 mL | |
| 40 mM | 0.0711 mL | 0.3557 mL | 0.7114 mL | 1.7785 mL | |
| 50 mM | 0.0569 mL | 0.2846 mL | 0.5691 mL | 1.4228 mL | |
| 60 mM | 0.0474 mL | 0.2371 mL | 0.4743 mL | 1.1857 mL |
BRD-6929 Related Classifications
HY-100719 Related Classifications
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