GSK3368715 (trihydrochloride)

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].

Product Specifications

CAS Number

[2227587-26-8]

Product Name Alternative

EPZ019997 (trihydrochloride)

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk3368715-trihydrochloride.html

Solubility

10 mM in DMSO

Smiles

CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl.Cl

Molecular Formula

C20H41Cl3N4O2

Molecular Weight

475.92

References & Citations

[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.