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Histone acetyltransferase (HAT) inhibitors target the writers of lysine acetylation on histones and other proteins. Acetylation neutralizes the positive charge of histone tails and favors transcription. In 1996 a Tetrahymena HAT was found to be related to a yeast transcriptional regulator, which linked histone acetylation to gene activation. In the same year the coactivators p300 and CREB-binding protein (CBP) were shown to be histone acetyltransferases. C646, found in 2010 by virtual ligand screening, is a selective inhibitor of the p300/CBP HAT domain. MG149 and NU 9056 target lysine acetyltransferase 5 (KAT5, Tip60), and garcinol is a natural product with broad HAT inhibition. SGC-CBP30 and I-CBP112 bind the CBP/p300 bromodomain rather than the catalytic site.
JQAD1 is a CRBN-dependent PROTAC selectively targeting EP300 for degradation. It effectively reduces EP300 protein levels and H3K27ac histone acetylation, resulting in apoptosis. JQAD1 is a valuable tool for investigating EP300 function and epigenetic regulation in cellular processes.
JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation.
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy.
