MS8815 (C09-1153-636)

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)In VitroMS8815 shows potency in inhibiting the EZH2 and EZH1 methyltransferase activity with IC 50 values of 8.6 nM and 62 nM, respectively. MS8815 (0.1-1 μM) degrades EZH2 with a DC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MDA-MB-453 cells and BT549 cells Concentration: 0.3, 3 μM; 1μM Incubation Time: 48 h; 24 h Result: Induced nearly complete degradation of EZH2 and exhibited the most robust degradation at 0.3 μM. Induced EZH2 degradation in a time-and concentration-dependent manner. Induced EZH2 degradation through the UPS. Cell Proliferation AssayCell Line: BT549, MDA-MB-468, SUM159 and MDA-MB-453 cells Concentration: 0.1-10 μM Incubation Time: 5 days Result: Showed superior cellular growth inhibition activity in a panel of TNBC cells.IC50& Target:IC50: 8.6 nM (EZH2),62 nM (EZH1),DC50: 140 nM (EZH2 in MDA-MB-453 cells). Specifications and Purity: 10mM in DMSO. Molecular Formula: C65H87N9O8S. Molecular Weight: 1154.51.