2108899-91-6

Gcn5 is a chromatin modifying factor whose HAT activity is required to acetylate histone H3 lysine 9 (K9) and K14, which facilitates transcription elongation by relaxing nucleosomes. CPTH2 inhibits the HAT activity of Gcn5 both in vitro and in vivo, reducing histone H3K14 acetylation at a concentration of 0.8 mM. It is a useful tool to study the impact of Gcn5-dependent acetylation in various biological systems and recently has been used to control the replication of human adenovirus.

CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].

GCN5

[1] Cocco E, et al. KAT3B-p300 and H3AcK18/H3AcK14 levels are prognostic markers for kidney ccRCC tumoraggressiveness and target of KAT inhibitor CPTH2. Clin Epigenetics. 2018 Apr 4;10:44. DOI:10.1186/s13148-018-0473-4
[2] Chimenti F, et al. A novel histone acetyltransferase inhibitor modulating Gcn5 network: cyclopentylidene-[4-(4'-chlorophenyl)thiazol-2-yl)hydrazone. J Med Chem. 2009 Jan 22;52(2):530-6. DOI:10.1021/jm800885d