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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
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