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GSK3368715 (dihydrochloride)
$120 – $980
Products Details
Product Description
– GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity[1].
Web ID
– HY-128717A
Storage Temperature
– 4°C (Powder, stored under nitrogen)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C20H40Cl2N4O2
Citations
– 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.|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.
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
– 1628925-77-8
Molecular Weight
– 439.46
Compound Purity
– 99.94
SMILES
– CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– DMSO : 230 mg/mL (ultrasonic)|H2O : 140 mg/mL (ultrasonic)
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.
