GSK3368715
Based on 19 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.
For research use only. We do not sell to patients.
- Purity: 99.41%
- CAS No.: 1629013-22-4
- Formula: C20H38N4O2
- Molecular Weight:366.54
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Storage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK3368715
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]
- FASEB J. 2025 Jan 15;39(1):e70293. [Abstract]
- Transl Oncol. 2025 Jan 3:52:102264. [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.
Customer Validation & Images
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WB
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Cell Proliferation/Viability Assay
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In Vivo Efficacy Study
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WB
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WB
All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT1 |
PRMT4 |
PRMT3 |
PRMT6 |
PRMT8 |
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
38.25 μM
Compound: 6; GSK3368715
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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
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[PMID: 38460270] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1629013-22-4
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Appearance Oil
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Molecular Weight 366.54
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Formula C20H38N4O2
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Color Colorless to light yellow
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SMILES
CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C
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Synonyms
EPZ019997
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 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).
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Nat Chem Biol
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).
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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 -
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 -
Transl Oncol
TNG908 is a brain-penetrant, MTA-cooperative PRMT5 inhibitor developed for the treatment of MTAP-deleted cancers. [Abstract]2025 Jan 3:52:102264. PMID: 39756156 -
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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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
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