MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder ; Blue, CRBN ligand ; Black, Linker 7).
MS181 (compound 1) (0, 0.1, 0.3, 1, 3, 10 µM; 24 h) decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B in a dose dependent manner[1].
MS181 (50 mg/kg; i.p.; once) shows bioavailable in mice[1].
References:
[1]. Kabir M, et al. Discovery and Characterization of a Novel Cereblon-Recruiting PRC1 Bridged PROTAC Degrader. J Med Chem. 2024 Apr 25;67(8):6880-6892.