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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-BRD4884
BRD4884

Chemical Structure : BRD4884

CAS No.: 1404559-91-6

BRD4884 (BRD 4884)

货号: PC-72672Not For Human Use, Lab Use Only.

BRD4884 is a potent, kinetically selective HDAC2 inhibitor with IC50 of 29/62 nM for HDAC1/2, >17-fold selectivity versus HDAC3.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BRD4884 is a potent, kinetically selective HDAC2 inhibitor with IC50 of 29/62 nM for HDAC1/2, >17-fold selectivity versus HDAC3.
BRD4884 shows slow-on/slow-off kinetics for HDAC2, but a shift to fast-on/faster-off kinetics for HDAC1, leading to a 7-fold longer half-life on HDAC2 (T 1/2 143 min) versus HDAC1 (T 1/2 20 min). This binding profile provides kinetic selectivity for HDAC2 and good thermodynamic selectivity for HDAC1, 2 versus HDAC3.
BRD4884 produced significant increases in AcH4K12 and AcH3K9 in mouse forebrain primary neuronal cultures.
BRD4884 (10 mg/kg) rescued the memory defects associated with p25 induced neurodegeneration in a murine model of neurodegeneration.

物理化学性质&存储条件

分子量 314.4
分子式 C18H19FN2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-amino-4'-fluoro[1,1'-biphenyl]-3-yl)tetrahydro-2H-pyran-4-carboxamide

参考文献

1. F F Wagner, et al. Chem Sci. 2015 Jan 1;6(1):804-815.

2. Wagner FF, et al. Bioorg Med Chem. 2016 Sep 15;24(18):4008-4015.

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