Cat. No. Name Size Price Add Cart
KI2118EPZ-567610 mg$432
EPZ-567650 mg$1552

Chemical Characteristic

Product NameEPZ-5676
SynonymsN/A
CAS No.1380288-87-8
Molecular Weight 562.71
FormulaC30H42N8O3
Chemical Name9-(5-deoxy-5-((cis-3-(2-(6-(1,1-dimethylethyl)-1h-benzimidazol-2-yl)ethyl)cyclobutyl)(1-methylethyl)amino)-beta-d-ribofuranosyl)-9h-purin-6-amine
SmilesO1[C@H]([C@@H]([C@@H]([C@H]1CN(C(C)C)C1CC(C1)CCc1[nH]c2c(n1)cc(cc2)C(C)(C)C)O)O)n1cnc2c1ncnc2N
Chemical Structure

Biological activities

EPZ-5676 is a potent and selective inhibitor of DOT1L methyltransferase with a Ki value of 80 pM. EPZ-5676 shows 37,000-fold selectivity against all other tested methyltransferases. In vitro in MV4-11 cells, EPZ-5676 inhibits H3K79 dimethylation with an IC50 of 2.6 nM.[1]

References

[1] Robert A Copeland, et al. Protein methyltransferases in cancer. 2013. AACR Annual Meeting.

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