CPI-1612

P300/CBP-IN-6 is a p300/CBP histone acetyltransferase (HAT) inhibitor extracted from patent WO2019161162A1, compound 33, has an IC50 of 330 nM for p300 HAT[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Acetyltransferase

IC50: 330 nM (p300 HAT)[1]

Histone acetyltransferases (HATs) catalyze the acetylation (transfer of an acetyl group) on a e-amino group of a target lysine side chain within a substrate histone, and histone deacetylases (HDACs) catalyze the removal of acetyl groups from lysine residues. Subsequently, acetylated core histones were shown to preferentially associate with transcriptionally active chromatin. HATs are categorized into four major families based on primary sequence homology, shared structural features, and functional roles: Gcn5/PCAF (General control nonrepressed protein 5 and p300 and CBP associated factor); MYST (named for the founding members MOZ, Ybf2/Sas3, Sas2, and Tip60); p300/CBP (protein of 300kDa and CREB Binding Protein); and Rttl09 (Regulator of Tyl Transposition gene production 109)[1].

[1]. Jonathan E. Wilson, et al. P300/cbp hat inhibitors. WO2019161162A1.