MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC 50 value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC).
MS8815 shows potency in inhibiting the EZH2 and EZH1 methyltransferase activity with IC50 values of 8.6 nM and 62 nM, respectively.MS8815 (0.1-1 μM) degrades EZH2 with a DC50 value of 140 nM in MDA-MB-453 cells.MS8815 (1 μM; 48 h) induces robust EZH2 degradation in a concentration-, time-, and proteasome-dependent manner in TNBC cells.MS8815 (0.1-10 μM; 5 days) effectively suppresses the cell growth in multiple TNBC cell lines and primary patient TNBC cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Brandon Dale, et al. Targeting Triple-Negative Breast Cancer by a Novel Proteolysis Targeting Chimera Degrader of Enhancer of Zeste Homolog 2. ACS Pharmacol Transl Sci. 2022 Jun 24;5(7):491-507.
溶解度数据
In Vitro: DMSO : 120 mg/mL (103.94 mM; Need ultrasonic)配制储备液