PROTAC EZH2 Degrader-3

PROTAC EZH2 Degrader-3 (compound ZJ-20) is a EZH2 PROTAC degrader. PROTAC EZH2 Degrader-3 (5 μM, 24 h) not only potently inhibits the expression of EZH2 protein, but also had a strong inhibits effect on the expression levels of other subunits of PRC2 as well as H3k27me3 protein. PROTAC EZH2 Degrader-3 shows anti-proliferative activity and blocks the cell cycle in the G0-G1 phase and induces cell apoptosis ((Blue: cereblon ligand Pomalidomide (HY-10984), Black: linker HY-W361751; Pink: EZH2 inhibitor Tazemetostat (HY-13803) ) [1].

Product Specifications

CAS Number

[3098718-46-5]

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase; PROTACs

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-ezh2-degrader-3.html

Smiles

CCN(C1CCOCC1)C2=CC(C3=CC=C(CN4CCN(C(CC5CCC(CNC6=C(C(N(C7C(NC(CC7)=O)=O)C8=O)=O)C8=CC=C6)CC5)=O)CC4)C=C3)=CC(C(NCC9=C(C)C=C(C)NC9=O)=O)=C2C

Molecular Formula

C56H68N8O8

Molecular Weight

981.19

References & Citations

[1]Fu M, et al. Chemically induced degradation of PRC2 complex by EZH2-Targeted PROTACs via a Ubiquitin-Proteasome pathway. Bioorg Med Chem Lett. 2024;113:129968.