GSK3368715 trihydrochloride

Names

[ Name ]:
GSK3368715 trihydrochloride

Biological Activity

[Description]:

GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Histone Methyltransferase

[Target]

PRMT4:1148 nM (IC50)

PRMT3:48 nM (IC50)

PRMT1:3.1 nM (IC50)

PRMT6:5.8 nM (IC50)

PRMT8:1.7 nM (IC50)

[In Vitro]

GSK3368715 trihydrochloride (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types[1].

[In Vivo]

GSK3368715 trihydrochloride (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively[1].

[References]

[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715 trihydrochloride, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₄₁Cl₃N₄O₂

[ Molecular Weight ]:
475.92

[ Storage condition ]:
-20°C

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.