PROTAC EZH2 Degrader-2

• UNSPSC Description:

  PROTAC EZH2 Degrader-2 (compound E-3P-MDM2), an EZH2 inhibitor, is a PROTAC composed of Tazemetostat (EPZ6438) and an E3 ligase system ligand. PROTAC EZH2 Degrader-2 degrades EZH2 in SU-DHL-6 cells in a dose-dependent manner, inhibits the expression of H3K27me3, and simultaneously degrades EED and SUZ12 proteins without affecting their mRNA levels. PROTAC EZH2 Degrader-2 has anti-cancer and anti-proliferative activity[1].

• Target Antigen:

  Histone Methyltransferase; PROTACs

• Type:

  Reference compound

• Related Pathways:

  Epigenetics;PROTAC

• Applications:

  Cancer-programmed cell death

• Field of Research:

  cancer

• Assay Protocol:

  https://www.medchemexpress.com/protac-ezh2-degrader-2.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  CC1=CC(C)=C(CNC(C2=CC(C3=CC=C(CN4CCN(C(C5=CN(CCOCCOCCOCCNC(CN6CCN(C(N7C(C8=CC=C(OC)C=C8OC(C)C)=N[C@H](C9=CC=C(Cl)C=C9)[C@@H]7C%10=CC=C(Cl)C=C%10)=O)CC6=O)=O)N=N5)=O)CC4)C=C3)=CC(N(C%11CCOCC%11)CC)=C2C)=O)C(N1)=O

• Molecular Weight:

  1463.55

• References & Citations:

  [1]Xie H et al. Design, synthesis and evaluation of EZH2-based PROTACs targeting PRC2 complex in lymphoma. Bioorg Chem. 2023 Nov;140:106762.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  No Development Reported