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].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase

Related Pathways

Apoptosis; Epigenetics

Field of Research

Cancer

Smiles

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

Molecular Formula

C29H43N7O6

Molecular Weight

585.70

References & Citations

[1]Daigle SR, et al. Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor. Cancer Cell. 2011 Jul 12;20 (1) :53-65.|[2]Chen L, et al. Abrogation of MLL-AF10 and CALM-AF10-mediated transformation through genetic inactivation or pharmacological inhibition of the H3K79 methyltransferase Dot1l. Leukemia. 2013 Apr;27 (4) :813-22.|[3]Deshpande AJ, et al. Leukemic transformation by the MLL-AF6 fusion oncogene requires the H3K79 methyltransferase Dot1l.Blood. 2013 Mar 28;121 (13) :2533-41.