PROTAC EZH2 Degrader-3

PROTAC EZH2 Degrader-3 (ZJ-20) potently inhibits proliferation of MINO cells with an IC₅₀ of 5.0 nM and OCI-LY7 cells with an IC₅₀ of 150 nM^[1].
PROTAC EZH2 Degrader-3 (5.0 μM; 24 h) potently degrades all core subunits of the PRC2 complex and reduces H3K27me3 levels in MINO cells^[1].
PROTAC EZH2 Degrader-3 (5.0 μM; 24 h) activates the mitochondrial apoptosis pathway in MINO cells by up-regulating pro-apoptotic proteins and down-regulating anti-apoptotic proteins^[1].
PROTAC EZH2 Degrader-3 (5.0 μM; 24 h) directly binds to EZH2 protein (increasing its thermal stability by 5-10 °C) but does not directly bind to other PRC2 complex subunits in MINO cells^[1].
PROTAC EZH2 Degrader-3 (0.02-20.0 μM; 24 h) induces dose-dependent degradation of EZH2 protein in MINO cells, with near-complete degradation at 5.0 μM after 24 h^[1].
PROTAC EZH2 Degrader-3 binds firmly to the EZH2-EED protein complex via hydrogen bonds with ASN-191, LYS-211, and TYR-111, with its Pomalidomide moiety positioned to recruit E3 ubiquitin ligase^[1].
PROTAC EZH2 Degrader-3 (5.0 μM; 24 h) arrests 79.47% of MINO cells in the G0-G1 phase of the cell cycle^[1].
PROTAC EZH2 Degrader-3 (5.0 μM; 24 h) induces apoptosis in 62.44% of MINO cells, which is 1.92 times more potent than Tazemetostat^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.