Background
PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.
PROTAC BET Degrader-1 (Compound 9) is a potent BET degrader based on PROTAC, decreases the level of BRD2, BRD3, and BRD4 proteins in RS4;11 cells at 3-10 nM, and inhibits the growth of this cell line with an IC50 of 4.3 nM, and 45.5 nM for MOLM-13 cells[1].
[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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