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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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