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EPZ 6438
- Tazemetostat
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C34H44N4O4
- MW: 572.74
Description
EPZ 6438 (Tazemetostat) is a potent, selective and orally bioavailable EZH2 inhibitor with reported IC50 values of 2–38 nM in EZH2 enzymatic assays. It reduces H3K27 trimethylation and induces apoptosis and differentiation in SMARCB1-deleted malignant rhabdoid tumor cells.
EZH2 is the catalytic PRC2 methyltransferase that maintains repressive H3K27 methylation and oncogenic chromatin states. EPZ 6438 is relevant for epigenetic oncology and EZH2-dependent tumor vulnerability research.
Key Features
- Potent EZH2 enzymatic inhibitor
- Orally bioavailable epigenetic oncology scaffold
- Reduces intratumoral H3K27 trimethylation
- Induces apoptosis and differentiation in SMARCB1-deleted models
Applications
- EZH2 activity assays
- H3K27 methylation studies
- Malignant rhabdoid tumor research
- Epigenetic therapy model profiling
More Information
| Parent CAS No. | 1403254-99-8 |
|---|---|
| Chemical Name | N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide |
| SMILES | C1(C2=CC=C(CN3CCOCC3)C=C2)=CC(N(CC)C2CCOCC2)=C(C)C(C(NCC2=C(C)C=C(C)NC2=O)=O)=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40) |
| InChiKey | NSQSAUGJQHDYNO-UHFFFAOYSA-N |
| CID | 66558664 |
| Short Description | EZH2 HMTase inhibitor |
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