2. Cell Cycle/DNA Damage Epigenetics Anti-infection
  3. HDAC HIV
  4. BRD-6929

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.

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BRD-6929

BRD-6929 構造式

CAS 番号 : 849234-64-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 82 在庫あり
Solution
10 mM * 1 mL in DMSO USD 82 在庫あり
Solid
5 mg $75 在庫あり
10 mg $120 在庫あり
25 mg $250 在庫あり
50 mg $400 在庫あり
100 mg $610 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 3 publication(s) in Google Scholar

Other Forms of BRD-6929:

BRD-6929 関連抗体

Top Publications Citing Use of Products

HDAC アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

HIV アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
HIV HIV-1 HIV-2

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

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[3].

IC50 & Target[1][3]

HDAC1

1 nM (IC50)

HDAC2

8 nM (IC50)

HDAC3

458 nM (IC50)

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
Epithelial cell IC50
>50 μM
Compound: 19
Cytotoxicity against human mammary epithelial cells by MTT assay
Cytotoxicity against human mammary epithelial cells by MTT assay
[PMID: 17941625]
HCT-116 GI50
0.11 μM
Compound: 60
Antiproliferative activity against human HCT116 cells assessed as cell viability
Antiproliferative activity against human HCT116 cells assessed as cell viability
[PMID: 18182289]
HCT-116 IC50
0.5 μM
Compound: 19
Cytotoxicity against human HCT116 cells by MTT assay
Cytotoxicity against human HCT116 cells by MTT assay
[PMID: 17941625]
Jurkat CC50
12.6 μM
Compound: 1; TPB
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
[PMID: 29541372]
Jurkat IC50
204 nM
Compound: 1
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
[PMID: 24405391]
Jurkat IC50
40 nM
Compound: 1
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
[PMID: 24405391]
KB IC50
5.27 μM
Compound: SHI1:2
Cytotoxicity against human KB cells after 72 hrs by MTS assay
Cytotoxicity against human KB cells after 72 hrs by MTS assay
[PMID: 25899338]
Sf9 IC50
0.001 μM
Compound: 60
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
[PMID: 27377864]
Sf9 IC50
0.013 μM
Compound: 60
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
[PMID: 27377864]
U-937 CC50
14 μM
Compound: 1; TPB
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
[PMID: 29541372]
体外実験

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.

BRD-6929 関連抗体
体内実験

BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a Cmax, T1/2 and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a Cmax, T1/2 and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain[1].
BRD-6929 (intraperitoneal injection; 45 mg/kg; 10 days) acts as a deacetylase inhibitor in mouse brain. It significantly increases acetylation in each brain region by 1.5- to 2.0-fold compared to vehicle. The western blotting reveals that BRD-6929 significantly increases acetylation of histone H2B (tetra-acetylated), H3K9 and H4K12 in cortex, ventral striatum and hippocampus after the 10th daily treatment in adult male C57BL/6J mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

351.42

分子式

C19H17N3O2S
CAS 番号
Appearance

Solid

Color

Off-white to gray

SMILES

O=C(NC1=CC(C2=CC=CS2)=CC=C1N)C3=CC=C(NC(C)=O)C=C3
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8456 mL 14.2280 mL 28.4560 mL
5 mM 0.5691 mL 2.8456 mL 5.6912 mL
10 mM 0.2846 mL 1.4228 mL 2.8456 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
純度とドキュメンテーション

純度: 99.01%

COA (247 KB) HNMR (142 KB) LCMS (389 KB)

取扱説明書 (2659 KB)
参考文献

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
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BRD-6929 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BRD-6929849234-64-6BRD6929BRD 6929HDACHIVHistone deacetylasesHuman immunodeficiency virusmood-relatedbehavioralHDACiInhibitorinhibitorinhibit

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製品名:
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製品番号:
HY-100719
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