For research use only. Not for therapeutic Use.
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].
| Catalog Number | I040267 |
| Synonyms | 5-[4-[[4-[1-[2-[2-[2-[2-[[2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetyl]amino]ethoxy]ethoxy]ethoxy]ethyl]triazole-4-carbonyl]piperazin-1-yl]methyl]phenyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methylbenzamide |
| Molecular Formula | C77H93Cl2N13O12 |
| Purity | ≥95% |
| InChI | InChI=1S/C77H93Cl2N13O12/c1-8-91(61-23-33-100-34-24-61)67-43-58(42-64(53(67)6)74(95)81-45-65-51(4)41-52(5)82-75(65)96)55-11-9-54(10-12-55)46-86-26-28-87(29-27-86)76(97)66-47-90(85-84-66)32-36-102-38-40-103-39-37-101-35-25-80-69(93)48-88-30-31-89(49-70(88)94)77(98)92-72(57-15-19-60(79)20-16-57)71(56-13-17-59(78)18-14-56)83-73(92)63-22-21-62(99-7)44-68(63)104-50(2)3/h9-22,41-44,47,50,61,71-72H,8,23-40,45-46,48-49H2,1-7H3,(H,80,93)(H,81,95)(H,82,96)/t71-,72+/m1/s1 |
| InChIKey | RRDJNHBEROQEFR-KPBBBUKSSA-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)C(=O)C6=CN(N=N6)CCOCCOCCOCCNC(=O)CN7CCN(CC7=O)C(=O)N8C(C(N=C8C9=C(C=C(C=C9)OC)OC(C)C)C1=CC=C(C=C1)Cl)C1=CC=C(C=C1)Cl |
| Reference | [1]. Xie H et al. Design, synthesis and evaluation of EZH2-based PROTACs targeting PRC2 complex in lymphoma. Bioorg Chem. 2023 Nov;140:106762. |
