Background
HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is employed for the design of potential PROTAC BET degrader. Antitumor activity[1].
HJB97 is a highly potent and efficacious bomodomain and extra terminal (BET) inhibitor with IC50s of 3.1±0.7 nM (BRD2 BD1), 3.9±0.5 nM (BRD2 BD2), 6.6±0.2 nM (BRD3 BD1), 1.9±0.4 nM (BRD3 BD2), 7.0±0.6 nM (BRD4 BD1), 7.0±0.1 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±5.3 nM and 25.6±1.9 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].|| Cell Viability Assay[1]||Cell 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 IC50s 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 Analysis[1]||Cell 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.
[1]. Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.
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