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GSK4028

Names

[ CAS No. ]:
2079886-19-2

[ Name ]:
GSK4028

Biological Activity

[Description]:

GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.

[Related Catalog]:

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain
Signaling Pathways >> Epigenetics >> Histone Acetyltransferase
Research Areas >> Inflammation/Immunology
Research Areas >> Cancer

[Target]

pIC50: 4.9 (PCAF/GCN5)[1].


[In Vitro]

GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9. GSK4028 also demonstrates potency toward BRD4 BD1 and BRD9 inTR-FRET assay with pIC50s of <4.3 and 4.5±0.13, respectively[1].

[References]

[1]. Humphreys PG, et al. Discovery of a Potent, Cell Penetrant, and Selective p300/CBP-Associated Factor (PCAF)/General Control Nonderepressible 5 (GCN5) Bromodomain Chemical Probe. J Med Chem. 2017 Jan 26;60(2):695-709.


[Related Small Molecules]

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15

Chemical & Physical Properties

[ Molecular Formula ]:
C17H21BrN4O

[ Molecular Weight ]:
377.28

[ Storage condition ]:
2-8℃


Related Compounds