1. Epigenetics
  2. Histone Methyltransferase
  3. GSK3368715

GSK3368715 (Synonyms: EPZ019997)

Cat. No.: HY-128717
Handling Instructions

GSK3368715 (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 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.

For research use only. We do not sell to patients.

GSK3368715 Chemical Structure

GSK3368715 Chemical Structure

CAS No. : 1629013-22-4

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Description

GSK3368715 (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 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1].

IC50 & Target

IC50: 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)[1]
Kiapp: 1.5 nM (PRMT1), 81 nM (PRMT3), 19 nM (PRMT4), 2.4 nM (PRMT6), 2 nM (PRMT8)[1]

In Vitro

GSK3368715 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK3368715 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

366.54

Formula

C20H38N4O2

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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GSK3368715
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HY-128717
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