2098545-98-1
Chemical Structure
Zeprumetostat
- CAS No.: 2098545-98-1
- Formula:C32H44N4O4
- Molecular Weight:548.72
IUPAC Name: N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-ethyl-6-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-(piperidin-1-ylmethyl)benzofuran-4-carboxamide
InChIKey: YLZVNQZYAYVUCW-UHFFFAOYSA-N
SMILES: O=C1NC(C)=CC(C)=C1CNC(C2=C3C=C(CN4CCCCC4)OC3=CC(N(C5CCOCC5)CC)=C2CC)=O
Biological Activity: Zeprumetostat is an orally active EZH2 inhibitor. Zeprumetostat inhibits wild-type and Y641F mutant EZH2 with IC50 values of 0.87 nM and 2.68 nM, respectively. Zeprumetostat induces cell cycle arrest and apoptosis, inhibits tumor cell proliferation, reduces target protein levels, and modulates oncogenic signaling pathway genes. Zeprumetostat combined with Tucidinostat (HY-109015) enhances antitumor efficacy through STAT1 and inhibits tumor growth in xenograft models. Zeprumetostat can be used for lymphoma-related research[1][2][3].
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Zeprumetostat | 99.18% | Zeprumetostat is an orally active EZH2 inhibitor. Zeprumetostat inhibits wild-type and Y641F mutant EZH2 with IC50 values of 0.87 nM and 2.68 nM, respectively. Zeprumetostat induces cell cycle arrest and apoptosis, inhibits tumor cell proliferation, reduces target protein levels, and modulates oncogenic signaling pathway genes. Zeprumetostat combined with Tucidinostat (HY-109015) enhances antitumor efficacy through STAT1 and inhibits tumor growth in xenograft models. Zeprumetostat can be used for lymphoma-related research. | ||||||||||||||||||||
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Similarity Score 0.80
HY-111418EBI-2511 -
Similarity Score 0.64
HY-156615Igermetostat -
Similarity Score 0.63
HY-13803RTazemetostat (Standard) -
Similarity Score 0.63
HY-147230EZH2-IN-13 -
Similarity Score 0.61
HY-179351EZH2 ligand-1 -
Similarity Score 0.60
HY-149726EZH2-IN-17 -
Similarity Score 0.60
HY-185582EZH2 ligand-4 -
Similarity Score 0.59
HY-786945-Bromo-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-2-methylbenzamide -
Similarity Score 0.59
HY-147091Tazemetostat de(methyl morpholine)-COOH -
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References
- [1]. Wu J, et al. EZH2 inhibitor SHR2554 enhances the anti-tumor efficacy of HDAC inhibitor Chidamide through STAT1 in T-cell lymphoma. Cell Death & Disease, 2025, 16: 522.
- [2]. Tan Z, et al. Design, synthesis and antiproliferative activity of pyridone derivatives as potent enhancer of zeste homologue 2/histone deacetylase dual inhibitors. RSC advances. 2026 Sep 03;16(40):46752-46762.
- [3]. Keam S J. Zeprumetostat: First Approval. Drugs, 2026, 86: 391-396.