GSK3368715 trihydrochloride
Based on 19 publication(s) in Google Scholar
GSK3368715 trihydrochloride (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 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity.
For research use only. We do not sell to patients.
- CAS No.: 2227587-26-8
- Formula: C20H41Cl3N4O2
- Molecular Weight:475.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Publications Citing Use of MedChemExpress (MCE) GSK3368715 trihydrochloride
More- Clin Mol Hepatol. 2026 Apr;32(2):843-865. [Abstract]
- Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
- Nat Chem Biol. 2024 Dec;20(12):1566-1576. [Abstract]
- Sci Adv. 2023 Sep 8;9(36):eadi2232. [Abstract]
- Cell Death Dis. 2021 Nov 13;12(11):1080. [Abstract]
- Cell Rep. 2024 Aug 22;43(9):114662. [Abstract]
- Cell Rep. 2023 Mar 29;42(4):112316. [Abstract]
- Front Pharmacol. 2020 Sep 8:11:569661. [Abstract]
- Transl Oncol. 2025 Feb:52:102264. [Abstract]
- FASEB J. 2025 Jan 15;39(1):e70293. [Abstract]
- Mol Carcinog. 2023 Aug;62(8):1119-1135. [Abstract]
- Bone Rep. 2023 Jul 25:19:101704. [Abstract]
- bioRxiv. 2026 May 29.
- University of Washington. 2025.
- Patent. US20240261260A1.
- Research Square Print. 26 Oct, 2022
- University of Munich. 2022 Oct.
- Research Square Print. September 20th, 2022.
- Research Square Preprint. 2022 Jul.
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All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT4 1148 nM (IC50) |
PRMT3 48 nM (IC50) |
PRMT1 3.1 nM (IC50) |
PRMT6 5.8 nM (IC50) |
PRMT8 1.7 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2227587-26-8
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Molecular Weight 475.92
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Formula C20H41Cl3N4O2
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SMILES
CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl.Cl
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Synonyms
EPZ019997 trihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (19)
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Journal Impact Factor
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Most Recent
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Clin Mol Hepatol
PRMT1-mediated asymmetric dimethylation of arginine residue 602 in DDX1 promotes cholangiocarcinoma progression. [Abstract]2026 Apr;32(2):843-865. PMID: 41668296 -
Nat Commun
PHGDH arginine methylation by PRMT1 promotes serine synthesis and represents a therapeutic vulnerability in hepatocellular carcinoma. [Abstract]2023 Feb 23;14(1):1011. PMID: 36823188
GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
PRMT1 inhibitor GSK3368715 (2 μM) markedly reduced the growth of HCC cells in vitro.
GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
Images, weight, and volume of Huh7 tumor xenografts from BALB/c nude mice fed with a -SG diet and treated with or without GSK3368715 (100 mg/kg; p.o.; every other day).
GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
GSK3368715 (2 μM; 6 h) blocked the binding of nonmethylated peptide with PRMT1 in Huh7 and PLC/PRF/5 cells.
GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]
Endogenous PHGDH was immunoprecipitated in Huh7 and PLC/PRF/5 cells treated with or without the PRMT1 inhibitor GSK3368715 (2 μM).
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Nat Chem Biol
2024 Dec;20(12):1566-1576. PMID: 39414979
GSK3368715 trihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1566-1576. [Abstract]
Immunoblot analysis and quantification of GSK3β-SNAP in MrTAC-treated HEK293T cells (10 μM; 3 h) in the presence of GSK368715 (10 μM).
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Sci Adv
Vitamin B6 is governed by the local compartmentalization of metabolic enzymes during growth. [Abstract]2023 Sep 8;9(36):eadi2232. PMID: 37682999 -
Cell Death Dis
PRMT1-mediated EZH2 methylation promotes breast cancer cell proliferation and tumorigenesis. [Abstract]2021 Nov 13;12(11):1080. PMID: 34775498 -
Cell Rep
CRISPR screening identifies PRMT1 as a key pro-ferroptotic gene via a two-layer regulatory mechanism. [Abstract]2024 Aug 22;43(9):114662. PMID: 39178116 -
Cell Rep
2023 Mar 29;42(4):112316. PMID: 36995937 -
Front Pharmacol
2020 Sep 8:11:569661. PMID: 33013410 -
Transl Oncol
TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]2025 Feb:52:102264. PMID: 39756156 -
FASEB J
PRMT1-mediated BRD4 arginine methylation and phosphorylation promote partial epithelial-mesenchymal transformation and renal fibrosis. [Abstract]2025 Jan 15;39(1):e70293. PMID: 39775984 -
Mol Carcinog
PRMT1 inhibition promotes ferroptosis sensitivity via ACSL1 upregulation in acute myeloid leukemia. [Abstract]2023 Aug;62(8):1119-1135. PMID: 37144835 -
Bone Rep
Protein arginine methyltransferases PRMT1, PRMT4/CARM1 and PRMT5 have distinct functions in control of osteoblast differentiation. [Abstract]2023 Jul 25:19:101704. PMID: 37593409 -
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Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GSK3368715 trihydrochloride Related Classifications
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