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CM-579

Names

[ CAS No. ]:
1846570-40-8

[ Name ]:
CM-579

Biological Activity

[Description]:

CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Epigenetics >> Histone Methyltransferase
Signaling Pathways >> Epigenetics >> DNA Methyltransferase

[Target]

DNA Methyltransferase:32 nM (IC50)

DNMT1:1.5 nM (Kd)

DNMT3A:92 nM (IC50)

DNMT3B:1000 nM (IC50)

G9a:16 nM (IC50)


[In Vitro]

The Kd of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC50s of 92 nM and 1000 nM, respectively[1].

[References]

[1]. San José-Enériz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424.

Chemical & Physical Properties

[ Molecular Formula ]:
C29H40N4O3

[ Molecular Weight ]:
492.65

[ Storage condition ]:
2-8℃

Related Compounds