Histone Acetyltransferases

L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM.

P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor.

GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50?=?1?nM, MYC EC50?=?18?nM), and it exhibits a good pharmacokinetic profile.

TH1834 dihydrochloride is a selective inhibitor of Tip60 (KAT5), a histone acetyltransferase involved in the regulation of gene expression and DNA repair. This compound has been shown to induce apoptosis and enhance DNA damage in breast cancer cells, demonstrating its potential as a therapeutic agent in cancer research. Importantly, TH1834 dihydrochloride does not inhibit the activity of the structurally related histone acetyltransferase MOF, suggesting a targeted approach in modulating histone acetylation and cellular responses.