GSK3368715 (Synonyms: EPZ019997) |
| Catalog No.GC36191 |
GSK3368715 (EPZ019997) est un inhibiteur de la protéine arginine méthyltransférase (PRMT) de type I actif par voie orale, réversible et S-adénosyl-L-méthionine (SAM) non compétitif (IC50 = 3,1 nM (PRMT1), 48 nM (PRMT3), 1148 nM ( PRMT4), 5,7 nM (PRMT6), 1,7 nM (PRMT8)). GSK3368715 (EPZ019997) produit un changement dans les états de méthylation de l'arginine, modifie l'utilisation des exons et possède une forte activité anticancéreuse.
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Cas No.: 1629013-22-4
Sample solution is provided at 25 µL, 10mM.
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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: 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]
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].
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].
[1]. Fedoriw A, et al. Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.
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