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JQ-1 is a triazolothienodiazepine compound that inhibits the BET bromodomain (BRD) family of proteins. Although it is a diazepine-like compound, JQ-1 exhibits no sedative or anxiolytic efficacy. JQ-1 was initially in development as a non-hormonal male contraceptive, inhibiting bromodomain testis-specific protein BRDT and chromatin remodeling during spermatogenesis, therefore preventing sperm production. This compound also activates latent HIV-1 in vitro and inhibits T cell proliferation through downregulation of T cell activation signals CD3, CD28, and CXCR4, JQ-1 is currently used as an experimental tool for examining mechanisms of HIV-1 latency. Additionally, JQ-1 exhibits anticancer chemotherapeutic activity in vitro and in vivo, through its inhibition of BRD4, JQ-1 suppresses Myc expression, IL-7R expression, and reduces JAK/STAT phosphorylation, inducing cell cycle arrest and prolonging cancer in a variety of cell lines. Biological bromodomain binding activity comes primarily from (+)-JQ-1, the (-)-JQ-1 stereoisomer does not bind BET bromodomains.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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