GSK4027 New
Data Sheet
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| CAS No. | 2079896-25-4 | Cat. No. | BCP25140 |
| Name | GSK4027 | ||
| Synonyms | GSK 4027;GSK-4027; | ||
| SMILES | CN1CC(CC(C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3 | ||
| Chemical Name | |||
| Formula | C17H21BrN4O | M. Wt | 377.28 |
| Purity | Storage | Store at 4-8°C | |
| Description | 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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