| Bioactivity | YM281 is a potent EZH2 inhibitor. YM281 induces cell apoptosis and cell cycle arrest at the G0/G1 phase. YM281 shows antitumor effects in vivo. YM281 has the potential for the research of lymphoma[1]. |
| Invitro | YM281 (compound V2) (0-6 µM; 0-48 h) decreases the EZH2 protein level and the PRC2 (polycomb repressive complex 2) complex through the VHL (vonHippel−Lindau)-dependent ubiquitin-proteasome system[1].YM281 (0-10 µM; 24 h) shows anticancer effects in lymphoma cells[1].YM281 (0-5 µM) induces cell apoptosis and cell cycle arrest at the G0/G1 phase[1].YM281 (0-5 µM; 24 h) increases the activity of caspase-3 and -7 and meanwhile reduces the cell viability in primary lymphoma cells[1]. Western Blot Analysis[1] Cell Line: |
| In Vivo | YM281 (80, 100 mg/kg; i.v.; 6 times for 3 weeks) shows antitumor effects and significantly reduces the expression of EZH2 protein and H3K27me3 levels[1]. Animal Model: |
| Name | YM281 |
| CAS | 2230914-84-6 |
| Formula | C56H71N7O9S |
| Molar Mass | 1018.27 |
| 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]. Tu Y,et al. Design, Synthesis, and Evaluation of VHL-Based EZH2 Degraders to Enhance Therapeutic Activity against Lymphoma. J Med Chem. 2021 Jul 22;64(14):10167-10184. |