PROTAC EZH2 Degrader-1

• CAT Number: I043512
• CAS Number: 2641601-67-2
• Molecular Formula: C54H67N7O8
• Molecular Weight: 942.15
• Purity: ≥95%
• Synonyms: N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-5-[4-[[4-[7-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyheptyl]piperazin-1-yl]methyl]phenyl]-3-[ethyl(oxan-4-yl)amino]-2-methylbenzamide
• InChI: InChI=1S/C54H67N7O8/c1-5-60(41-20-28-68-29-21-41)46-32-40(31-43(37(46)4)50(63)55-33-44-35(2)30-36(3)56-51(44)64)39-16-14-38(15-17-39)34-59-25-23-58(24-26-59)22-9-7-6-8-10-27-69-47-13-11-12-42-49(47)54(67)61(53(42)66)45-18-19-48(62)57-52(45)65/h11-17,30-32,41,45H,5-10,18-29,33-34H2,1-4H3,(H,55,63)(H,56,64)(H,57,62,65)
• InChIKey: LONVYJSHGSZBQY-UHFFFAOYSA-N
• SMILES: CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=CC=CC7=C6C(=O)N(C7=O)C8CCC(=O)NC8=O

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].

Reference

[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.
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