Potent and selective BET bromodomain inhibitor (IC50 values of 77 nM and 33 nM for inhibition of binding of a tetra-acetylated histone H4 peptide to BRD4 with the first and second bromodomain, respectively). (+)-JQ1 is capable of blocking the macrophage inflammatory responses via inhibition of BET proteins in mice, and activating HIV latency through antagonizing Brd4 inhibition of Tat-transactivation. Cotreatment with (+)-JQ1 and the FLT3 inhibitor AC220 (Axon 1696) synergistically induce apoptosis of cultured and primary CD34(+) human AML blast progenitor cells (BPC) expressing FLT3-ITD.

KEYWORDS: (+)-JQ1 | BET inhibitor | JQ1 | JQ-1 | JQ 1 | CAS [1268524-70-4] | Histone | BET (BRD) | Inhibitor | Proteins | Bromodomain | inflammatory | HIV latency