Art. -Nr.: HY-128717

GSK3368715

Name: GSK3368715
Brand: MedChemExpress
SKU: HY-128717
Price: 150.00 USD
Availability: InStock
Rating: 5 (21 reviews)

(Synonyms: EPZ019997)

21 Cited Publications

Kundenbewertung

Based on 21 publication(s) in Google Scholar

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.

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Reinheit : 99.41%
CAS. Nr.: 1629013-22-4
Formel: C₂₀H₃₈N₄O₂
Molecular Weight:366.54

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK3368715 Chemical Structure

CAS. Nr.: 1629013-22-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (21)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PRMT1

PRMT4

PRMT3

PRMT6

PRMT8

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	38.25 μM Compound: 6; GSK3368715	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth by CCK-8 assay	[PMID: 38460270]

In Vitro

GSK3368715 (EPZ019997) shows 50% or more growth inhibition relative to DMSO-treated cells in the majority of 249 cancer cell lines, representing 12 tumor types^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GSK3368715 (EPZ019997) significantly effects on the growth of BxPC3 xenografts at all doses tested, reducing tumor growth by 78% and 97% in the 150- and 300-mg/kg dose groups, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1629013-22-4
Appearance Oil
Molecular Weight 366.54
Formel C₂₀H₃₈N₄O₂
Color Colorless to light yellow
SMILES

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

EPZ019997
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (21)

All Cell Proliferation/Viability AssayIn Vivo Efficacy StudyWB

Sort by:

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 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 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 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 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 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

Protein tyrosine kinase-6 is post-translationally regulated by arginine methylation and ubiquitination. [Abstract]

2026 Jun 5;17(1):706. PMID: 42248824
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
University of California, Irvine

2026 Jun 3.
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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 5 mg/mL (13.64 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7282 mL

13.6411 mL

27.2822 mL

5 mM

0.5456 mL

2.7282 mL

5.4564 mL

10 mM

0.2728 mL

1.3641 mL

2.7282 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.83 mg/mL (2.26 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)

Verweise

[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]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7282 mL	13.6411 mL	27.2822 mL	68.2054 mL
	5 mM	0.5456 mL	2.7282 mL	5.4564 mL	13.6411 mL
	10 mM	0.2728 mL	1.3641 mL	2.7282 mL	6.8205 mL

Bioz

Keywords

GSK3368715

21 Cited Publications

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GSK3368715

Publications Citing Use of MedChemExpress (MCE) GSK3368715

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen