GSK4027

CAS NO.：2079896-25-4
Empirical Formula: C17H21BrN4O
Molecular Weight: 377.28
MDL number: MFCD31692324
Update Date: 2026-08-20 20:20:01

What is GSK4027?

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.

in vitro

Herein, this study reports GSK4027 as a chemical probe for the PCAF/GCN5 bromodomain, together with GSK4028 as an enantiomeric negative control._x000D_ _x000D_ Reference: J Med Chem. 2017 Jan 26;60(2):695-709. https://pubmed.ncbi.nlm.nih.gov/28002667/

Properties of GSK4027

Boiling point:	450.3±55.0 °C(Predicted)
Density	1.45±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO:50.0(Max Conc. mg/mL);132.53(Max Conc. mM)
form	A crystalline solid
pka	9.58±0.10(Predicted)
color	Light yellow to yellow

Safety information for GSK4027

Computed Descriptors for GSK4027

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