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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-GSK2801
GSK2801

Chemical Structure : GSK2801

CAS No.: 1619994-68-1

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GSK2801 (GSK 2801)

货号: PC-22925Not For Human Use, Lab Use Only.

GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains with KD values of 136 and 257 nM for BAZ2B and BAZ2A, respectively.

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

生物&药学活性

GSK2801 is a potent, selective and cell active acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains with KD values of 136 and 257 nM for BAZ2B and BAZ2A, respectively.
GSK2801 shows only low micromolar residual activity at BRD9 and TAF1L.
GSK2801 displaces full length GFP-BAZ2A from chromatin at concentrations below 1 μM in U2OS cells.
GSK2801 is a versatile tool compound for cellular and in vivo studies to understand the role of BAZ2 bromodomains in chromatin biology.

物理化学性质&存储条件

分子量 371.45
分子式 C20H21NO4S
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

1-(1-(2-(Methylsulfonyl)phenyl)-7-propoxyindolizin-3-yl)ethanone

参考文献

1. Chen P, et al. J Med Chem. 2016 Feb 25;59(4):1410-24.

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