EPZ020411 hydrochloride
Based on 10 publication(s) in Google Scholar
EPZ020411 hydrochloride is a selective inhibitor of PRMT6 with an IC50 of 10 nM, it has >10 folds selectivity for PRMT6 over PRMT1 and PRMT8. EPZ020411 hydrochloride can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 98.15%
- CAS No.: 2070015-25-5
- Formula: C25H39ClN4O3
- Molecular Weight:479.06
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Storage:
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
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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) EPZ020411 hydrochloride
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Brain. 2024 Jul 5;147(7):2552-2565. [Abstract]
- J Immunother Cancer. 2025 Mar 13;13(3):e010639. [Abstract]
- Cell Death Dis. 2023 Oct 9;14(10):655. [Abstract]
- Acta Pharmacol Sin. 2022 Feb;43(2):457-469. [Abstract]
- J Transl Med. 2025 Jan 16;23(1):74. [Abstract]
- J Transl Med. 2024 Oct 10;22(1):922. [Abstract]
- EMBO Rep. 2018 Dec;19(12):e46377. [Abstract]
- Bioorg Chem. 2024 May 10:148:107439. [Abstract]
- Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
All Histone Methyltransferase Isoforms
More
Biological Activity
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PRMT6 0.01 μM (IC50) |
PRMT1 0.119 μM (IC50) |
PRMT8 0.223 μM (IC50) |
EPZ020411 hydrochloride (0-20 μM; 24 h) decreases H3R2 methylation in A375 cells[1]. EPZ020411 hydrochloride (20-40 μM; 6 h) reduces neomycin- and cisplatin-induced cell apoptosis and increases hair cell survival[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells
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Concentration:0-20 μM
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Incubation Time:24 hours
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Result:Dose-dependently decreased H3R2 methylation in A375 cells with an IC50 of 0.634 μM.
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Cell Line:Cultured cochleae cells
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Concentration:20 and 40 μM
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Incubation Time:6 hours
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Result:Suppressed the apoptotic cascade induced by aminoglycosides and also inhibited cisplatin-induced apoptosis in the hair cells of the cochlear explants after pretreatment deposed. Reduced hair cell loss caused by cisplatin treatment.
| Rats IV 1 mg/kg |
Rats SC 5 mg/kg |
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| CL (mL/min/kg) | 19.7±1.0 | |
| Vss (L/kg) | 11.1±1.6 | |
| t1/2 (h) | 8.54±1.43 | 9.19±1.60 |
| tmax (h) | 0.444 | |
| Cmax (ng/mL) | 844±306 | |
| AUC0-τ (h·ng/mL) | 745±34 | 2456±135 |
| AUC0-inf (h·ng/mL) | 846±45 | 2775±181 |
| F (%) | 65.6±4.3 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J wild-type mice at P28 with acute ototoxicity model[2]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection; 10 mg/kg once
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Result:Significantly reduced neomycin- and cisplatin-induced HC loss and showed no effect without neomycin injection with mice.
Chemical Information
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CAS No. 2070015-25-5
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Appearance Solid
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Molecular Weight 479.06
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Formula C25H39ClN4O3
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Color Off-white to light yellow
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SMILES
CNCCN(C)CC1=CNN=C1C2=CC=C(O[C@H]3C[C@H](OCCC4CCOCC4)C3)C=C2.Cl[H]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, stored under nitrogen
* In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Brain
HSV-1 reactivation results in post-herpetic neuralgia by upregulating Prmt6 and inhibiting cGAS-STING. [Abstract]2024 Jul 5;147(7):2552-2565. PMID: 38366606 -
J Immunother Cancer
Protein arginine methyltransferase 6 enhances immune checkpoint blockade efficacy via the STING pathway in MMR-proficient colorectal cancer. [Abstract]2025 Mar 13;13(3):e010639. PMID: 40086819 -
Cell Death Dis
2023 Oct 9;14(10):655. PMID: 37813837 -
Acta Pharmacol Sin
2022 Feb;43(2):457-469. PMID: 33850273 -
J Transl Med
2025 Jan 16;23(1):74. PMID: 39819457 -
J Transl Med
KLF4 regulates trophoblast function and associates with unexplained recurrent spontaneous abortion. [Abstract]2024 Oct 10;22(1):922. PMID: 39390495 -
EMBO Rep
2018 Dec;19(12):e46377. PMID: 30420520 -
Bioorg Chem
Discovery of a first-in-class degrader for the protein arginine methyltransferase 6 (PRMT6). [Abstract]2024 May 10:148:107439. PMID: 38754310 -
Exp Cell Res
PRMT6 functionally associates with PRMT5 to promote colorectal cancer progression through epigenetically repressing the expression of CDKN2B and CCNG1. [Abstract]2022 Nov 16;422(1):113413. PMID: 36400182
EPZ020411 hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2022 Nov 16;422(1):113413. [Abstract]
EPZ020411(PRMT6i; 200-1000 nM) in combination with GSK591(PRMT5i; 200-1000 nM) exhibits a synergistic anti-proliferative effect on HCT116 and SW620 cells.
Solvent & Solubility
DMSO : 50 mg/mL (104.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
0.1 M HCl : 50 mg/mL (104.37 mM; ultrasonic and warming and adjust pH to 2 with HCl and heat to 60°C)
H2O : 20 mg/mL (41.75 mM; ultrasonic and warming and heat to 60°C)
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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
* 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: ≥ 2.5 mg/mL (5.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (280 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
[1]. Mitchell LH, et al. Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 ToolCompound. ACS Med Chem Lett. 2015 Apr 6;6(6):655-659. [Content Brief]
[2]. He Y, et al. Inhibition of Protein arginine methyltransferase 6 reduces reactive oxygen species production and attenuates aminoglycoside- and cisplatin-induced hair cell death. Theranostics. 2020 Jan 1;10(1):133-150. [Content Brief]
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, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO / 0.1 M HCl | 1 mM | 2.0874 mL | 10.4371 mL | 20.8742 mL | 52.1855 mL |
| 5 mM | 0.4175 mL | 2.0874 mL | 4.1748 mL | 10.4371 mL | |
| 10 mM | 0.2087 mL | 1.0437 mL | 2.0874 mL | 5.2186 mL | |
| 15 mM | 0.1392 mL | 0.6958 mL | 1.3916 mL | 3.4790 mL | |
| 20 mM | 0.1044 mL | 0.5219 mL | 1.0437 mL | 2.6093 mL | |
| 25 mM | 0.0835 mL | 0.4175 mL | 0.8350 mL | 2.0874 mL | |
| 30 mM | 0.0696 mL | 0.3479 mL | 0.6958 mL | 1.7395 mL | |
| 40 mM | 0.0522 mL | 0.2609 mL | 0.5219 mL | 1.3046 mL | |
| DMSO / 0.1 M HCl | 50 mM | 0.0417 mL | 0.2087 mL | 0.4175 mL | 1.0437 mL |
| 60 mM | 0.0348 mL | 0.1740 mL | 0.3479 mL | 0.8698 mL | |
| 80 mM | 0.0261 mL | 0.1305 mL | 0.2609 mL | 0.6523 mL | |
| 100 mM | 0.0209 mL | 0.1044 mL | 0.2087 mL | 0.5219 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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