BRD 6929;COMPOUND-60
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- CAS号:
- 849234-64-6
- 英文名:
- 4-acetamido-N-(2-amino-5-(thiophen-2-yl)phenyl)benzamide
- 英文别名:
- 151025;Merck60;BRD 6929;Compound-60;BRD 6929;COMPOUND-60;4-Acetamido-N-[2-amino-5-(2-thienyl)phenyl]benzamide;4-acetamido-N-(2-amino-5-(thiophen-2-yl)phenyl)benzamide;Benzamide, 4-(acetylamino)-N-[2-amino-5-(2-thienyl)phenyl]-;Inhibitor,mood-related,BRD-6929,Human immunodeficiency virus,HDAC,BRD6929,HDACi,BRD 6929,HIV,behavioral,inhibit,Histone deacetylases
- 中文名:
- BRD 6929;COMPOUND-60
- 中文别名:
- 化合物BRD-6929;4-乙酰氨基-N-[2-氨基-5-(2-噻吩基)苯基]苯甲酰胺
- CBNumber:
- CB93380135
- 分子式:
- C19H17N3O2S
- 分子量:
- 351.42
- MOL File:
- 849234-64-6.mol
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BRD 6929;COMPOUND-60化学性质
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储存条件:
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Store at -20°C
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溶解度:
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DMSO: soluble
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形态:
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A solid
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BRD 6929;COMPOUND-60性质、用途与生产工艺
BRD-6929 是 I 类组蛋白去乙酰化酶 HDAC1 和 HDAC2 的脑渗透性选择性抑制剂 (IC50= 1 和 8 nM)。BRD-6929 对 HDAC1 和 HDAC2 有高亲和力 (Ki = 0.2 和 1.5 nM)。BRD-6929 可用于情绪相关行为的研究。
HDAC1
1 nM (IC
50
)
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HDAC2
8 nM (IC
50
)
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HDAC3
458 nM (IC
50
)
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HIV-1
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In vitro IC
50
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 IC
50
s of 0.001 µM, 0.008 µM, 0.458 µM and >30 µM, respectively.
In vitro binding affinity (K
i
) and kinetics (half-life ‘T
1/2
′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 µM), the K
i
values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T
1/2
values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively.
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).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 EC
50
of 7.2 µM in cultured neurons.BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1.
BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a C
max
, T
1/2
and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a C
max
, T
1/2
and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain.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.
BRD 6929;COMPOUND-60
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-100719 | BRD 6929;COMPOUND-60 BRD-6929 | 849234-64-6 | 1mg | 342元 |
2024/04/30 | HY-100719 | BRD 6929;COMPOUND-60 BRD-6929 | 849234-64-6 | 5mg | 900元 |
BRD 6929;COMPOUND-60
生产厂家
849234-64-6, BRD 6929;COMPOUND-60 相关搜索:
- 抑制剂
- 标准品
- 4-乙酰氨基-N-[2-氨基-5-(2-噻吩基)苯基]苯甲酰胺
- 化合物BRD-6929
- 849234-64-6
- 4-Acetamido-N-[2-amino-5-(2-thienyl)phenyl]benzamide
- Inhibitor,mood-related,BRD-6929,Human immunodeficiency virus,HDAC,BRD6929,HDACi,BRD 6929,HIV,behavioral,inhibit,Histone deacetylases
- Benzamide, 4-(acetylamino)-N-[2-amino-5-(2-thienyl)phenyl]-
- Merck60
- 151025
- Compound-60
- BRD 6929;COMPOUND-60
- BRD 6929
- 4-acetamido-N-(2-amino-5-(thiophen-2-yl)phenyl)benzamide