NCIt synonyms : BET Inhibitor CC-90010; 4-(2-(Cyclopropylmethoxy)-5-methylsulfonylphenyl)-2-methylisoquinolin-1-one;
NCIt definition : An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family
of proteins, with potential antineoplastic activity. Upon oral administration, trotabresib
preferentially binds to the second bromodomain (BD2) of BET proteins, thereby preventing
the interaction between the BET proteins and acetylated histones. This disrupts chromatin
remodeling and gene expression. Prevention of the expression of certain growth-promoting
genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells.
BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that contain
two homologous bromodomains, the BD1 and BD2 domains. They play an important role
during development and cellular growth.;
UNII : K424WH3WU0;
CAS number : 1706738-98-8; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 1706738-98-8
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