cbp/p300-in-5

P300/CBP-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase (IC50 of 18.8 nM).

GSK702 是一种 PROTAC，是 GSK983 的顺式-(S,S)-对映体，活性较低。GSK702 仅轻微降低 PCAF 蛋白水平，并通过与 CRBN 结合减少巨噬细胞中的 IL-1β。该化合物适用于炎症介质研究。

Selective p300 histone acetyltransferase (HAT) inhibitor (IC50 = 50-500 nM). Exhibits approximately 100-fold selectivity for p300 over PCAF (IC50 = 200 μM). Inhibits p300-dependent transcription. Active in vivo. Lau et al (2000) HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol.Cell. 5 589 PMID:10882143 |Liu et al (2008) The structural basis of protein acetylation by the p300/CBP transcriptional coactivator. Nature. 451 846 PMID:18273021 |Burns et al (2005) Iso-coenzyme A. J.Biol.Chem. 280 16550 PMID:15708855 |Cebrat et al (2003) Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg.Med.Chem. 11 3307 PMID:12837541