PROTAC BET Degrader-1

PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Signaling Pathways >> PROTAC >> PROTAC

Research Areas >> Cancer

BET[1]

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.

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15