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GSK4027 结构式

GSK4027

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货号 :BCP25140CAS号 :2079896-25-4纯度:
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  • 基本信息与产品描述
CAS号 2079896-25-4 货号 BCP25140
中文名 GSK4027
英文名 GSK4027
中文别名
英文别名 GSK 4027;GSK-4027;
SMILES CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3
化学名称
分子式 C17H21BrN4O 分子量 377.28
纯度 配送 惯例下常温包邮
产品描述 GSK4027 is a potent and selective chemical probe for the PCAF/GCN5 bromodomain. GSK4027 has PCAF TR-FRET pIC50 = 7.4 ; PCAF BROMOscan pKi = 8.9; GCN5 BROMOscan pKi = 8.9; PCAF NanoBRET pIC50 =7.2; BRD4 BD1 TR-FRET pIC50 < 4.3. GSK4027 shows high potency for the PCAF/GCN5 bromodomain, high solubility, cellular target engagement, and ≥18000-fold selectivity over the BET family, together with ≥70-fold selectivity over the wider bromodomain families. p300/CREB binding protein associated factor (PCAF/KAT2B) and general control nonderepressible 5 (GCN5/KAT2A) are multidomain proteins that have been implicated in retroviral infection, inflammation pathways, and cancer development.
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