GSK3368715 dihydrochloride
Based on 19 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 1628925-77-8
- Formula: C20H40Cl2N4O2
- Molecular Weight:439.46
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Storage:
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
Publications Citing Use of MedChemExpress (MCE) GSK3368715 dihydrochloride
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.
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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All Histone Methyltransferase Isoforms
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Biological Activity
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PRMT1 |
PRMT4 |
PRMT3 |
PRMT6 |
PRMT8 |
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1628925-77-8
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Appearance Solid
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Molecular Weight 439.46
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Formula C20H40Cl2N4O2
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Color White to off-white
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SMILES
CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl
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Synonyms
EPZ019997 dihydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture)
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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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 dihydrochloride 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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Solvent & Solubility
DMSO : 200 mg/mL (455.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 140 mg/mL (318.57 mM; Need ultrasonic)
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, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.73 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (227.55 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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, 2 years; -20°C, 1 year (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.2755 mL | 11.3776 mL | 22.7552 mL | 56.8880 mL |
| 5 mM | 0.4551 mL | 2.2755 mL | 4.5510 mL | 11.3776 mL | |
| 10 mM | 0.2276 mL | 1.1378 mL | 2.2755 mL | 5.6888 mL | |
| 15 mM | 0.1517 mL | 0.7585 mL | 1.5170 mL | 3.7925 mL | |
| 20 mM | 0.1138 mL | 0.5689 mL | 1.1378 mL | 2.8444 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9102 mL | 2.2755 mL | |
| 30 mM | 0.0759 mL | 0.3793 mL | 0.7585 mL | 1.8963 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5689 mL | 1.4222 mL | |
| 50 mM | 0.0455 mL | 0.2276 mL | 0.4551 mL | 1.1378 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3793 mL | 0.9481 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7111 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2276 mL | 0.5689 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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