For research use only. Not for therapeutic Use.
EPZ011989(CAT: I002025) is a potent, selective, and orally bioavailable inhibitor of the histone methyltransferase EZH2, widely utilized in epigenetics and oncology research. It effectively targets EZH2-mediated H3K27 methylation, which plays a critical role in gene silencing and tumorigenesis. EPZ011989 is particularly valuable for studying cancers with EZH2 gain-of-function mutations, such as non-Hodgkin lymphoma, and other malignancies driven by epigenetic dysregulation. Its high specificity and efficacy make it a powerful tool for exploring therapeutic strategies, advancing drug discovery, and understanding the role of epigenetic modifications in disease progression.
Catalog Number | I002025 |
CAS Number | 1598383-40-4 |
Synonyms | N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-benzamide |
Molecular Formula | C₃₅H₅₁N₅O₄ |
Purity | ≥95% |
Target | Histone Methyltransferase |
Solubility | DMSO: ≥ 33 mg/mL |
Storage | -20°C |
IC50 | < 3 nM ( Ki for wt EZH2, EZH2 Y646) |
IUPAC Name | N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl-[4-[2-methoxyethyl(methyl)amino]cyclohexyl]amino]-2-methyl-5-(3-morpholin-4-ylprop-1-ynyl)benzamide |
InChI | InChI=1S/C35H51N5O4/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42) |
InChIKey | XQFINGFCBFHOPE-UHFFFAOYSA-N |
SMILES | CCN(C1CCC(CC1)N(C)CCOC)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C#CCN4CCOCC4 |