EPZ011989 hydrochloride

• CAT Number: I040510
• CAS Number: 2095432-26-9
• Molecular Formula: C35H52ClN5O4
• Molecular Weight: 642.27
• Purity: ≥95%
• Synonyms: 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;hydrochloride
• IUPAC Name: EPZ011989 hydrochloride is a potent and orally active Zeste Homolog 2 (EZH2) inhibitor, with a Ki value of <3 nM. EPZ011989 shows anti-tumor activity. EPZ011989 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups[1].
• InChI: InChI=1S/C35H51N5O4.ClH/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);1H
• InChIKey: LHRBDVKQGXCMQN-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.Cl

EPZ011989 hydrochloride(CAT: I040510) is a potent, orally active inhibitor of Enhancer of Zeste Homolog 2 (EZH2), a histone methyltransferase implicated in epigenetic gene silencing and cancer progression. With a Ki value of <3 nM, EPZ011989 effectively suppresses EZH2 enzymatic activity and demonstrates significant anti-tumor efficacy in preclinical models. This compound also features an alkyne functional group, enabling its use in bioorthogonal click chemistry applications via copper-catalyzed azide-alkyne cycloaddition (CuAAC). This dual functionality makes EPZ011989 ideal for target engagement studies, proteomic profiling, and selective labeling of EZH2-associated proteins. Supplied in high purity for advanced research in epigenetics and chemical biology.

Reference

[1]. Campbell JE, et al. EPZ011989, A Potent, Orally-Available EZH2 Inhibitor with Robust in Vivo Activity. ACS Med Chem Lett. 2015 Mar 4;6(5):491-495.
[Content Brief]