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GSK 4027

CAS No. : 2079896-25-4

MCE 站：GSK 4027

产品活性：GSK 4027 是一种 PCAF/GCN5 溴结构域的化学探针，作用于 PCAF，pIC₅₀ 为 7.4±0.11。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain  |  Histone Acetyltransferase

In Vitro: 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 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 pIC₅₀ 7.2 (IC₅₀ 60 nM).

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