SYN-3004 | CAS 1268524-70-4
The compound (+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor (IC50 values of 17.7, 32.6, 76.9 and 12942 nM respectively for BRD2 (N-terminal (N)), BRD4 (C-terminal (C)), BRD4 (N) and CREBBP respectively. In binding assays, (+)-JQ1 binds to BRD4 bromodomain 1 (Kd=50 nM) and and BRD4 bromodomain 2 (Kd= 90 nM). The binding is competitive with acetyl lysine, and (+)-JQ1 may be a useful chemical probe to investigate the role of BET bromodomains in the transcriptional regulation of oncogenesis. In other work, the compound JQ1 exhibited strong dose-and time- dependent inhibition of Bromodomain testis-specific protein or BRDT, a Bromodomain containing protein highly enriched in testis. BRDT is involved in chromatin remodeling and is essential for healthy sperm development. JQ1 appears to block that function and cause a decrease in sperm viability so the compound is being examined as a potential male contraceptive.