EPZ004777 (hydrochloride)

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

Product Specifications

CAS Number

[1380316-03-9]

UNSPSC

12352005

Target

Apoptosis; Histone Methyltransferase

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/epz004777-hydrochloride.html

Concentration

10mM

Purity

99.46

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

NC1=C2C(N([C@H]3[C@H](O)[C@H](O)[C@@H](CN(C(C)C)CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)O3)C=C2)=NC=N1.[H]Cl

Molecular Formula

C28H42ClN7O4

Molecular Weight

576.13

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.