NHWD-870 is an Orally Active and Selective BET Bromodomain Inhibitor
Brominedomain can recognize acetylated lysine residues. As the “reader” of lysine acetylation, the bromine domain is responsible for the transduction of signals carried by acetylated lysine residues and transforming them into various normal or abnormal phenotypes. Specifically, the bromine domain-containing proteins have a variety of functions. Besides, it ranges...
GNE-371, a Chemical Probe for the Second Bromodomains of TFIID Subunit 1 and TFIID Subunit 1-Like
Bromodomains are protein modules that serve as epigenetic readers. These modules consist of 110 amino acids, specifically recognize acetylated lysine residues on histone tails. They also play important roles in chromatin-structural changes and transcriptional regulation. A number of inhibitors of the bromodomain and extra terminal (BET) family and non-BET...
CC-90010 is a Reversible and Orally Active BET Inhibitor
Come straight to the point, CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. The bromodomain and extra-terminal domain (BET) proteins, epigenetic readers, recognize and bind acetylated lysine residues. The BET protein family comprises the ubiquitously expressed...
GNE-987, a BET PROTAC Degrader, is a Part of PROTAC-Antibody (CLL1) Conjugate for ADC
BRD4 is a member of the BET family of proteins (BRD2, 3, 4, and T). It functions as an epigenetic “reader” of acetylated histone lysine residues via its two bromodomain motifs (BD1 and BD2). Disruption of BRD4-histone interactions is an attractive strategy for the development of novel anti-cancer agents....
BETd-260 is a Potent PROTAC BET Degrader
The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...
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....
GSK778 is a Potent and Selective Inhibitor of BET BD1
The bromodomain is a protein domain of about 110 amino acids, which can recognize acetylated lysine residues. Specifically, the bet (Bromo- and terminal domain) family consists of germ cell-specific (BRDT) and ubiquitously expressed (BRD2, BRD3, Brd4) epigenetic reader proteins. As a “reader” of lysine acetylation, bromodomain is responsible for...