MS147 is a VHL-based PROTAC PRC1 degrader. It shows binding affinity (Kd) of 3.0 µM to EED and 450 nM to VHL. The compound selectively targets the EED protein, a crucial component of PRC2, through its EED ligand portion, and interacts with PRC1 core components BMI1 and RING1B. This interaction enables MS147 to recruit BMI1 and RING1B near VHL, leading to their degradation. As a result, MS147 reduces the ubiquitination level of H2AK119ub, thereby impacting the proliferation of cancer cells.
Formel:
C54H70N12O6S
Target-Kategorie:
E1/E2/E3 Enzyme|||PROTACs
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