GSK4027

Research use only, not for human use.

GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both.

GSK4027 (GSK 4027, GSK-4027) is a potent, selective, cell-penetrant chemical probe of PCAF/GCN5 bromodomain with pKi of 8.9 for both; displays exceptional selectivity over the BET bromodomain family (>18000-fold selectivity over the BET family, >70-fold selectivity over the wider bromodomain families) and proof of cellular target engagement; GSK4027 is a useful chemical tool in elucidating the biological phenotype of PCAF/GCN5 bromodomain inhibition.

GSK 4027 is a PCAF/GCN5 bromodomain chemical probe. 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. GSK 4027 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 5.1±0.08, respectively. The selectivity of GSK 4027 against the wider bromodomain family is assessed in the BROMOscan panel with pKi of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with Ki of 1.4 nM for both bromodomains. As expected due to the encouraging measured artificial membrane permeability (500 nm/s), treatment of HEK293 cells with GSK 4027 displace full length PCAF from histone H3.3 with little drop-off from the biochemical assay and a pIC50 7.2 (IC50 60 nM).

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GSK 4027 | GSK-4027

Chromatin/Epigenetic

Bromodomain

Bromodomain

Inflammation/Immunology

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2079896-25-4

377.286

C17H21BrN4O

>98% (HPLC)

DMSO : 50 mg/mL 132.53 mM

CN1C[C@@H](C2=CC=CC=C2)C[C@@H](NC3=C(Br)C(N(C)N=C3)=O)C1

4-Bromo-2-methyl-5-(((3R,5R)-1-methyl-5-phenylpiperidin-3-yl)amino)pyridazin-3(2H)-one

(-20℃)

With Ice Pack

≥ 2 years