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Product 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].
Web ID
– HY-128717
Shipping
– Room temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C20H38N4O2
Citations
– Bone Rep. 2023 Jul 25, 101704.|Mol Carcinog. 2023 May 5.|Research Square Print. 26 Oct, 2022|Research Square Print. September 20th, 2022.|University of Munich. Fakultät für Medizin. 2022 Oct.|Cell Death Dis. 2021 Nov 13;12(11):1080.|Cell Rep. 2023 Mar 29;42(4):112316.|Front Pharmacol. 2020 Sep 8;11:569661.|Mol Carcinog. 2023 May 5.|Nat Commun. 2023 Feb 23;14(1):1011.|Research Square Preprint. 2022 Jul.|Sci Adv. 2023 Sep 8;9(36):eadi2232.
References
– [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.
CAS Number
– 1629013-22-4
Molecular Weight
– 366.54
SMILES
– CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C
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.
