1380288-87-8

Uses

9-[5-Deoxy-5-[[cis-3-[2-[6-(1,1-dimethylethyl)-1H-benzimidazol-2-yl]ethyl]cyclobutyl](1-methylethyl)amino]-β-D-ribofuranosyl]-9H-purin-6-amine, can be used as an adenosine anticancer, and antibiotic analogues.

Biological Activity

epz5676 is a potent inhibitor of dot1l histone methyltransferase, according to x-ray crystallographic analysis, that occupies the s-adenosyl methionine (sam) binding pocket of dot1l and induces conformational changes in dot1l resulting in the opening of a hydrophobic pocket beyond the amino acid portion of sam. epz5676 selectively inhibits dotil with a value of 50% inhibition concentration ic50 of 0.8 nm, which is 37000-fold greater in selectivity than other methyltransferases, including carm1, ehmt1/2, ezh1/2, prmt1/2/5/6/8, setd7, smyd2/3, and whsc1/1l1. epz5676 has been investigated for the treatment of mll-rearranged leukemia in multiple studies where results have shown that epz5676 inhibits h3k79 methylation and the expression of mll-fusion target gene and potently kills acute leukemia cell lines bearing mll translocation.daigle sr, olhava ej, therkelsen ca, basavapathruni a, jin l, boriack-sjodin pa, allain cj, klaus cr, raimondi a, scott mp, waters nj, chesworth r, moyer mp, copeland ra, richon vm, pollock rm. potent inhibition of dot1l as treatment of mll-fusion leukemia. blood. 2013 aug 8;122(6):1017-1025.