AB3067 is a PROTAC degrader for BET protein , that recruits two different E3 ligase Cereblon and VHL with good affinity ( IC 50 =559 nM for VHL in live HEK293; IC 50 =190 nM for CRBN in live HEK293), and degrades BRD2 , BRD3 , BRD4 and CRBN with DC 50 of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC 50 of 111 nM. (Pink: ligand for target protein ; Black: linker ; Blue: ligand for E3 ligase VHL and CRBN)
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