DS17701585 is a Highly Selective, Orally Active EP300 and CBP Inhibitor
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.15, 0.040, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. Besides, DS17701585 has the potential for the research of cancer. EP300 and its paralog CBP play an important role in post-translational modification as...
DCH36_06 is a Selective p300/CBP Inhibitor
Histone acetyltransferases (HATs) are epigenetic enzymes that relieve transcriptional repression by preferentially acetylation of ε-amino group of lysine residues on histones. In general, HATs are crucial for chromatin restructuring and transcriptional regulation in eukaryotic cells. HATs can be grouped into at least five different subfamilies (HAT1, Gcn5/PCAF, MYST, p300/CBP,...
dCBP-1 is a Selective PROTAC Degrader of p300/CBP
The paralogous chromatin regulators CREB-binding protein (CBP) and p300 are factors critical for establishing and activating enhancer-mediated transcription. The CREB-binding protein (CBP) and p300 are important factors for activating enhancer-mediated transcription. These proteins consist of at least 10 distinct functional domains. Most of them interact with over 400 other proteins,...
NEO2734 is an Orally Active Dual p300/CBP and BET Bromodomain Selective Inhibitor
NUT midline carcinoma (NMC) is a rare, aggressive subtype of squamous carcinoma. This kind of cancer is usually driven by BRD4-NUT fusion oncoprotein. BRD4, a BET protein, binds to chromatin through its two bromodomains. At the same time, NUT recruits the p300 HAT to activate oncogenic target genes transcription....
GNE-207 is an Orally Active Inhibitor for the Bromodomain of CBP
Both CBP (Cyclic AMP response element binding protein, binding protein) and P300 (paralog E1A-associated protein of 300 kDa) possess several structured regions. As such, the histone acetyltransferase (HAT) domain is a common region. It acetylates both histone and non-histone proteins, and bromodomain (BRD) that binds acetylated lysine (KAc). In...