PROTAC EZH2 Degrader-1

PROTAC EZH2 Degrader-1 (Compound 150d), a potent PROTAC EZH2 Degrader, exerts inhibitory effect on EZH2 methyltransferase activity with the IC50 of 2.7 nM. EZH2 plays an important role in many tumorigenesis and development processes[1].

Product Specifications

CAS Number

[2641601-67-2]

UNSPSC

12352005

Target

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-1.html

Purity

99.44

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

CCN(C1CCOCC1)C2=C(C(C(NCC3=C(C=C(NC3=O)C)C)=O)=CC(C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=C7C(N(C(C7=CC=C6)=O)C8CCC(NC8=O)=O)=O)=C2)C

Molecular Formula

C54H67N7O8

Molecular Weight

942.15

References & Citations

[1]Juan Xia, et al. Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects. J Med Chem. 2022 May 26;65 (10) :7016-7043. |[2]Shi MX, et al., PROTAC EZH2 degrader-1 overcomes the resistance of podophyllotoxin derivatives in refractory small cell lung cancer with leptomeningeal metastasis. BMC Cancer. 2024 Apr 22;24 (1) :504.