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GSK3368715 (dihydrochloride)

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].

Product Specifications

CAS Number

[1628925-77-8]

Product Name Alternative

EPZ019997 (dihydrochloride)

UNSPSC

12352005

Target

Histone Methyltransferase

Type

Reference compound

Related Pathways

Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gsk3368715-dihydrochloride.html

Purity

99.96

Solubility

DMSO : 200 mg/mL (ultrasonic) |H2O : 140 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C20H40Cl2N4O2

Molecular Weight

439.46

References & Citations

[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, stored under nitrogen, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

PRMT1; PRMT3; PRMT4; PRMT6; PRMT8

Citation 01

Cell Death Dis. 2021 Nov 13;12 (11) :1080.|Cell Rep. 2023 Mar 29;42 (4) :112316.|Cell Rep. 2024 Aug 22;43 (9) :114662.|Front Pharmacol. 2020 Sep 8;11:569661.|Mol Carcinog. 2023 Aug;62 (8) :1119-1135.|Nat Chem Biol. 2024 Dec;20 (12) :1566-1576.|Nat Commun. 2023 Feb 23;14 (1) :1011.|Patent. US20240261260A1.|Research Square Preprint. 2022 Jul.|Sci Adv. 2023 Sep 8;9 (36) :eadi2232.|Transl Oncol. 2025 Jan 3:52:102264.|University of Washington. 2025.|Bone Rep. 2023 Jul 25:19:101704.|FASEB J. 2025 Jan 15;39 (1) :e70293.|Mol Carcinog. 2023 Aug;62 (8) :1119-1135.|Research Square Print. 26 Oct, 2022|Research Square Print. September 20th, 2022.|University of Munich. Fakultät für Medizin. 2022 Oct.

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