Uses
EPZ 004777 is potent small molecule inhibitor of protein lysine methyltransferase DOT1L.
Definition
ChEBI: 1-[3-[[(2R,3S,4R,5R)-5-(4-amino-7-pyrrolo[2,3-d]pyrimidinyl)-3,4-dihydroxy-2-oxolanyl]methyl-propan-2-ylamino]propyl]-3-(4-tert-butylphenyl)urea is a N-glycosyl compound.
Biological Activity
epz004777 is a specific small-molecule h3k79 methyltransferase dot1l inhibitor that potently inhibits dot1l in a radionuclide homogeneous assay with the half maximal inhibition concentration ic50 value of 400 pm and selectively kills a variety of mll-rearranged leukemia cells, including an mll-af4 leukemia cell line mv4-11 and an mll-af9 leukemia cell line molm13 [1 & 2].epz004777 has also been found to selectively inhibit the proliferation of mll-af10 and calm-af10 transformed cells in a dose dependent manner (ic50: 0.1 μm to 1 μm), in which the mrna expression levels of two hallmark leukemogenic genes (hoxa9 and meis1) are suppressed by epz004777 in a concentration dependent manner [2].
