EPZ004777 (formate)

EPZ004777 formate is an effective and selective DOT1L inhibitor, with IC50 being 0.4 nM. EPZ004777 formate reduces the levels of H3K79me2 and H3K79me1, significantly down-regulating the expression of HOXA9 and MEIS1. EPZ004777 formate selectively inhibits the proliferation of MLL rearrangement cells and promotes the differentiation and subsequent apoptosis (apoptosis) of leukemia cells. EPZ004777 formate can be used for the study of leukemia[1][2][3].

C29H43N7O6

585.7

O=CO.NC1=NC=NC2=C1C=CN2[C@H]3[C@H](O)[C@H](O)[C@@H](CN(C(C)C)CCCNC(NC(C=C4)=CC=C4C(C)(C)C)=O)O3

Apoptosis; Histone Methyltransferase

DOT1L

Room temperature