HJB97

HJB97 is a high-affinity BET inhibitor with K i s 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 is employed for the design of potential PROTAC BET degrader and has antitumor activity In Vitro HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC 50 s 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). HJB97 (10-1000 nM, 4 days) potently inhibits cell growth in RS4;11 and MOLM-13 acute leukemia cell lines with IC 50 s of 24.1 nM and 25.6 nM. 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). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: The human acute leukemia RS4;11 cell line; The human acute leukemia MOLM-13 cell line Concentration: 10-1000 nM Incubation Time: 4 days Result: Achieved IC 50 s value of 24.1±5.3 nM and 25.6±1.9 nM in inhibition of the RS4;11 cell and MOLM-13 cell growth. Western Blot AnalysisCell Line: RS4;11 cells Concentration: 30, 100, 300, 1000 nM Incubation Time: 24 h Result: Down-regulated the level of c-Myc but at concentrations of 300-1000 nM in the RS4;11 cell line. IC50& Target:BRD2 BD1 0.9±0.2 nM (Ki) BRD2 BD2 0.27±0.09 nM (Ki) BRD3 BD1 0.18±0.01 nM (Ki) BRD3 BD2 0.21±0.03 nM (Ki) BRD4 BD1 0.5±0.2 nM (Ki) BRD4 BD2 1.0±0.1 nM (Ki) BRD2 BD1 3.1±0.7 nM (IC 50 ) BRD2 BD2 3.9±0.5 nM (IC 50 ) BRD3 BD1 6.6±0.2 nM (IC 50 ) BRD3 BD2 1.9±0.4 nM (IC 50 ) BRD4 BD1 7.0±0.6 nM (IC 50 ) BRD4 BD2 7.0±0.1 nM (IC 50 )

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