Product Details
| Product Name:
BRD-6929 |
CAS No.:
849234-64-6 |
| Purity:
99.05% |
Supply Ability:
10g |
| Release date:
2024/11/14 |
Product Introduction
Bioactivity
| 名稱(chēng) | BRD-6929 |
| 描述 | BRD-6929 is a selective, brain-penetrant HDAC1 and HDAC2 inhibitor (IC50: ?1 and 8 nM). BRD-6929 (Cpd-60) shows high-affinity to HDAC1 and HDAC2 (Kis: 0.2 and 1.5 nM) [2]. BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1. BRD-6929 can be used for mood-related behavioral model research[3]. |
| 體外活性 | 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]. |
| 體內(nèi)活性 | BRD-6929, administered via intraperitoneal injection at a 45 mg/kg dosage, achieves peak plasma concentrations (Cmax) of 17.7 μM, has a half-life (T1/2) of 7.2 hours, and an area under the curve (AUC) of 25.6 μM/L*hr. In the brain, its Cmax, T1/2, and AUC are 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively. When given daily for 10 days at the same dose, BRD-6929 functions as a deacetylase inhibitor in mouse brain, elevating acetylation levels in various brain regions by 1.5- to 2.0-fold over the control. Specifically, it notably increases the acetylation of histone H2B (tetra-acetylated), H3K9, and H4K12 in the cortex, ventral striatum, and hippocampus of adult male C57BL/6J mice, as evidenced by western blotting after the 10th treatment[1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 4.9 mg/mL (14 mM), Sonication is recommended.
|
| 關(guān)鍵字 | Inhibitor | mood-related | Human immunodeficiency virus | BRD 6929 | HDAC | HDACi | HIV | behavioral | BRD6929 | inhibit | Histone deacetylases | BRD-6929 |
| 相關(guān)產(chǎn)品 | Stavudine | 5-Fluorouracil | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Sodium 4-phenylbutyrate | Dextran sulfate sodium salt (MW 4500-5500) | Lamivudine | Chloroquine phosphate | Curcumin | Decanedioic acid | Tenofovir |
| 相關(guān)庫(kù) | DNA 損傷和修復(fù)分子庫(kù) | 抗胰腺癌化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 染色質(zhì)修飾分子庫(kù) | 抗乳腺癌化合物庫(kù) | 抗病毒庫(kù) | 抑制劑庫(kù) | NO PAINS 化合物庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States