GSK 4027 (C09-1135-081)

GSK 4027 is a chemical probe for the PCAF / GCN5 bromodomain with an pIC 50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.In VitroGSK 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 pIC 50 s 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 pK i of 8.9 and 8.9 for PCAF and GCN5, respectively. GSK 4027 shows equipotent activity against PCAF and GCN5 with K i 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 pIC 50 7.2 (IC 50 60 nM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:pIC50: 7.4±0.11 (PCAF). Specification: 0.98 Molecular Formula: C17H21BrN4O Molecular Weight: 377.28 PubChem CID: 126961735 Isomeric SMILES: CN1C[C@H](C[C@H](C1)NC2=C(C(=O)N(N=C2)C)Br)C3=CC=CC=C3