Chemical Structure : EZM8266
CAS No.:
2140164-84-5
EZM8266
(EZM-8266)
Catalog No.: PC-28196Not For Human Use, Lab Use Only.
EZM8266 is a potent, selective and orally active G9a (histone lysine methyltransferase 2, EHMT2) inhibitor with IC50 of 1 pM for human EHMT2, effectively reduces H3K9me2 levels.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
EZM8266 is a potent, selective and orally active G9a (histone lysine methyltransferase 2, EHMT2) inhibitor with IC50 of 1 pM for human EHMT2, effectively reduces H3K9me2 levels.
EZM8266 binds to EHMT2 at the substrate binding site.
Combined with Olaparib is sufficient to induce regression of PARPi-resistant tumors and increase cytotoxic immune cells in the tumor microenvironment.
EZM8266 treatment markedly decreases colony formation, cell migration, and cell invasion in HCC.
EZM8266 enhances tumor cell immunogenicity and promotes immune-stimulatory pathways in HCC cells, potentiates the immunogenic effects of IFN-γ.
EZM8266 potentiates the in vivo antitumoral effect of ICI in HCC model developed by the orthotopic implantation of PM299L cells in immunocompetent mice.
Physicochemical Properties
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M.Wt
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373.46
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Formula
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C19H27N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-1-(azetidin-1-yl)-3-(2-methoxy-5-((4-methyl-6-(methylamino)pyrimidin-2-yl)amino)phenoxy)propan-2-ol
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References
1. Campbell JE, et al. Patent, WO2019079540 A. 2017-10-18 (Compound 5R).
2. Adan-Villaescusa E, et al. Cell Rep Med. 2026 Apr 21;7(4):102717.
3. Lily L Nguyen, et al. Mol Cancer Ther. 2024 Sep 1;23(9):1332–1347.
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