GSK3368715 (trihydrochloride)

SKU HY-128717B-Get quote Category Tags , ,

Products Details

Product 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].

Web ID

– HY-128717B

Shipping

– Room temperature

Molecular Formula

– C20H41Cl3N4O2

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.

CAS Number

– 2227587-26-8

Molecular Weight

– 475.92

SMILES

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

Clinical Information

– Phase 1

Research Area

– Cancer

Solubility

– 10 mM in DMSO

Target

– Histone Methyltransferase

Isoform

– PRMT1;PRMT3;PRMT4;PRMT6;PRMT8

Pathway

– Epigenetics

Product type

– Reference compound

Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.

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