| Bioactivity | 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 (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717)[1]. |
| Invitro | MS181 (compound 1) (0, 0.1, 0.3, 1, 3, 10 µM; 24 h) 以剂量依赖性方式降低 EED、EZH2、SUZ12、BMI1 和 RING1B 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> MS181 相关抗体: Western Blot Analysis[1] Cell Line: |
| In Vivo | MS181 (50 mg/kg; i.p.; once) 在小鼠体内具有生物利用度[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
| Formula | C39H41N11O6 |
| Molar Mass | 759.81 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |