HJB97

HJB97 is a high-affinity BET inhibitor with K_is of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), 1.0 nM (BRD4 BD2), respectively. HJB97 can be served as Ligands for Target Protein for PROTAC, employed for the design of potential PROTAC BET degrader and has antitumor activity^[1][2]. In Vitro:HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC₅₀s of 3.1 nM (BRD2 BD1), 3.9 nM (BRD2 BD2), 6.6 nM (BRD3 BD1), 1.9 nM (BRD3 BD2), 7.0 nM (BRD4 BD1), 7.0 nM (BRD4 BD2)^[1].
HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC₅₀s of 24.1 nM and 25.6 nM^[1].
HJB97 can effectively down-regulate the level of c-Myc at concentrations of 300-1000 nM in the RS4;11 cell line (treated for 24 h)^[1].