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Cat. No.: HY-128717C

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GSK3368715 hydrochloride

(Synonyms: EPZ019997 hydrochloride)

19 Cited Publications

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Based on 19 publication(s) in Google Scholar

GSK3368715 (EPZ019997) hydrochloride is an orally active, reversible, SAM-noncompetitive type I protein arginine methyltransferase (PRMT) inhibitor with IC₅₀ values of 3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), and 1.7 nM (PRMT8). GSK3368715 hydrochloride induces a shift in arginine methylation states, alters exon usage, and exhibits potent anticancer activity.

For research use only. We do not sell to patients.

CAS No.: 2227587-25-7
Formula: C₂₀H₃₉ClN₄O₂
Molecular Weight:403.00

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

GSK3368715 hydrochloride Chemical Structure

CAS No.: 2227587-25-7

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity

Description

All Histone Methyltransferase Isoforms :

Chemical Information

CAS No. 2227587-25-7
Molecular Weight 403.00
Formula C₂₀H₃₉ClN₄O₂
SMILES

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

EPZ019997 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (19)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWB

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Journal Impact Factor

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 hydrochloride 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 hydrochloride 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 hydrochloride 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 hydrochloride 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).
Nat Chem Biol

Methylarginine targeting chimeras for lysosomal degradation of intracellular proteins. [Abstract]

2024 Dec;20(12):1566-1576. PMID: 39414979

GSK3368715 hydrochloride 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).
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

CDK5-PRMT1-WDR24 signaling cascade promotes mTORC1 signaling and tumor growth. [Abstract]

2023 Mar 29;42(4):112316. PMID: 36995937
Front Pharmacol

Type I PRMT Inhibition Protects Against C9ORF72 Arginine-Rich Dipeptide Repeat Toxicity. [Abstract]

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
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.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

GSK3368715 hydrochloride

19 Cited Publications

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Biological Activity
- Description
Chemical Information
Publications (19)
Purity & Documentation
References

1/16
1/16

GSK3368715 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2024 Dec;20(12):1566-1576. [Abstract]

Customer Validation
Immunoblot analysis and quantification of GSK3β-SNAP in MrTAC-treated HEK293T cells (10 μM; 3 h) in the presence of GSK368715 (10 μM).
1/16

GSK3368715 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]

Customer Validation
PRMT1 inhibitor GSK3368715 (2 μM) markedly reduced the growth of HCC cells in vitro.
1/16

GSK3368715 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]

Customer Validation
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).
1/16

GSK3368715 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]

Customer Validation
GSK3368715 (2 μM; 6 h) blocked the binding of nonmethylated peptide with PRMT1 in Huh7 and PLC/PRF/5 cells.
1/16

GSK3368715 hydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2023 Feb 23;14(1):1011. [Abstract]

Customer Validation
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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GSK3368715 hydrochloride

Publications Citing Use of MedChemExpress (MCE) GSK3368715 hydrochloride

All Histone Methyltransferase Isoforms

Biological Activity

Chemical Information

Publications (19)

Purity & Documentation

References

Calculators

Help & FAQs

GSK3368715 hydrochloride Related Classifications

HY-128717C Related Classifications