EPZ015666
Based on 22 publication(s) in Google Scholar
EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 with an IC50 of 22 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.86%
- CAS No.: 1616391-65-1
- Formule: C20H25N5O3
- Masse moléculaire:383.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) EPZ015666
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Adv Sci (Weinh). 2025 Feb 3:e2415559. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 25;44(1):218. [Abstract]
- J Exp Clin Cancer Res. 2023 Aug 21;42(1):214. [Abstract]
- J Exp Clin Cancer Res. 2022 Oct 5;41(1):293. [Abstract]
- J Exp Clin Cancer Res. 2022 Jun 2;41(1):191. [Abstract]
- Sci Adv. 2024 Jun 7;10(23):eadm9589. [Abstract]
- Cancer Lett. 2024 Aug 30:217214. [Abstract]
- Cell Commun Signal. 2025 Mar 8;23(1):126. [Abstract]
- Acta Pharmacol Sin. 2023 Mar;44(3):573-583. [Abstract]
- J Med Chem. 2024 Sep 12;67(17):15098-15117. [Abstract]
- J Mol Cell Biol. 2026 Mar 11:mjag008. [Abstract]
- J Biol Chem. 2023 Aug;299(8):104964. [Abstract]
- J Biol Chem. 2022 Oct;298(10):102434. [Abstract]
- J Biol Chem. 2022 Sep;298(9):102367. [Abstract]
- J Proteome Res. 2024 Mar 1;23(3):1014-1027. [Abstract]
- PLoS One. 2023 Dec 22;18(12):e0296291. [Abstract]
- Biomed Res Int. 2021 Oct 19;2021:7329072. [Abstract]
- Exp Ther Med. 2021 Sep;22(3):1003. [Abstract]
- bioRxiv. 2026 Apr 13.
- Research Square Print. 2023 Feb.
- Patent. US20180263995A1.
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2D/3D Cell Culture and Differentiation
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WB
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Cell Proliferation/Viability Assay
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Others
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Histological Imaging/Staining
Voir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
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PRMT5 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.32 μM
Compound: EPZ015666
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38518523] |
| HCC38 | IC50 |
5 μM
Compound: 66; EPZ015666, GSK3235025
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Anticancer activity against human HCC38 cells assessed as cell growth inhibition by MTT assay
Anticancer activity against human HCC38 cells assessed as cell growth inhibition by MTT assay
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[PMID: 33650861] |
| HeLa | IC50 |
0.29 μM
Compound: EPZ015666
|
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38518523] |
| HepG2 | IC50 |
1.04 μM
Compound: EPZ015666
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38518523] |
| KARPAS-422 | IC50 |
0.96 μM
Compound: 8; EPZ015666
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Antiproliferative activity against human KARPAS422 cells after 4 days by cell titer-glo luminescent cell viability assay
Antiproliferative activity against human KARPAS422 cells after 4 days by cell titer-glo luminescent cell viability assay
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[PMID: 30366617] |
| Maver1 | IC50 |
450 nM
Compound: 1
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Antiproliferative activity against human Maver1 cells measured after 12 days post culturing by guava via count reagent assay
Antiproliferative activity against human Maver1 cells measured after 12 days post culturing by guava via count reagent assay
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[PMID: 29870258] |
| Maver1 | IC50 |
450 nM
Compound: 21; EPZ015666
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Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 12 days by Guava ViaCount Reagent Assay
Antiproliferative activity against human MAVER-1 cells assessed as cell growth inhibition incubated for 12 days by Guava ViaCount Reagent Assay
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[PMID: 37366223] |
| MCF7 | IC50 |
0.74 μM
Compound: EPZ015666
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38518523] |
| MDA-MB-231 | IC50 |
0.43 μM
Compound: EPZ015666
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by CCK-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth by CCK-8 assay
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[PMID: 38518523] |
| MDA-MB-231 | IC50 |
60 μM
Compound: 66; EPZ015666, GSK3235025
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Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation by MTT assay
Anticancer activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation by MTT assay
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[PMID: 33650861] |
| MDA-MB-468 | IC50 |
1 μM
Compound: 66; EPZ015666, GSK3235025
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Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition by MTT assay
Anticancer activity against human MDA-MB-468 cells assessed as cell growth inhibition by MTT assay
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[PMID: 33650861] |
| MV4-11 | GI50 |
0.106 μM
Compound: 1; EPZ015666
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Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 12 by Celltiter-glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 12 by Celltiter-glo luminescent cell viability assay
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[PMID: 30605830] |
| MV4-11 | GI50 |
0.212 μM
Compound: 1; EPZ015666
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Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 8 by Celltiter-glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells supplemented with fresh medium containing compound every 4 days measured on day 8 by Celltiter-glo luminescent cell viability assay
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[PMID: 30605830] |
| MV4-11 | IC50 |
1.8 μM
Compound: 8; EPZ015666
|
Antiproliferative activity against human MV4-11 cells after 4 days by cell titer-glo luminescent cell viability assay
Antiproliferative activity against human MV4-11 cells after 4 days by cell titer-glo luminescent cell viability assay
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[PMID: 30366617] |
| Pfeiffer | IC50 |
1.1 μM
Compound: 8; EPZ015666
|
Antiproliferative activity against human Pfeiffer cells after 4 days by cell titer-glo luminescent cell viability assay
Antiproliferative activity against human Pfeiffer cells after 4 days by cell titer-glo luminescent cell viability assay
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[PMID: 30366617] |
| SUD4 | IC50 |
2.6 μM
Compound: 8; EPZ015666
|
Antiproliferative activity against human SU-DHL4 cells after 4 days by cell titer-glo luminescent cell viability assay
Antiproliferative activity against human SU-DHL4 cells after 4 days by cell titer-glo luminescent cell viability assay
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[PMID: 30366617] |
| Z-138 | IC50 |
351 nM
Compound: EPZ015666; GSK3235025
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Antiproliferative activity against human Z138 cells incubated for 5 days by cell titer-glo assay
Antiproliferative activity against human Z138 cells incubated for 5 days by cell titer-glo assay
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[PMID: 26985292] |
| Z-138 | IC50 |
450 nM
Compound: 21; EPZ015666
|
Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 12 days by Guava ViaCount Reagent Assay
Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 12 days by Guava ViaCount Reagent Assay
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[PMID: 37366223] |
| Z-138 | IC50 |
96 nM
Compound: 1
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Antiproliferative activity against human Z138 cells measured after 12 days post culturing by guava via count reagent assay
Antiproliferative activity against human Z138 cells measured after 12 days post culturing by guava via count reagent assay
|
[PMID: 29870258] |
Treatment of MCL cell lines with EPZ015666 (GSK3235025) leads to inhibition of SmD3 methylation and cell death, with IC50 values in the nanomolar range[1]. EPZ015666 (GSK3235025), a potent peptide-competitive and SAM-cooperative inhibitor with >10,000-fold specificity against PRMT5 relative to other methyltransferases[2].
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. 1616391-65-1
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Appearance Solid
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Masse moléculaire 383.44
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Formule C20H25N5O3
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Color White to off-white
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SMILES
O=C(NC[C@H](O)CN1CCC(C=CC=C2)=C2C1)C3=CC(NC4COC4)=NC=N3
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Synonyms
GSK3235025
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (22)
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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 -
Adv Sci (Weinh)
PRMT5 Maintains Homeostasis of the Intestinal Epithelium by Modulating Cell Proliferation and Survival. [Abstract]2025 Feb 3:e2415559. PMID: 39899687
EPZ015666 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 3:e2415559. [Abstract]
EPZ015666 (2.5 μM). After treating the compound for 4 or 5 days, the number of shoots or surviving organoids was observed and quantified.
EPZ015666 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Feb 3:e2415559. [Abstract]
Indicated proteins were detected by immunoblotting in small intestinal organoids treated with vehicle (DMSO), EPZ015666 or LLY283 for 3 days.
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J Exp Clin Cancer Res
A novel polypeptide encoded by circSPIRE1 promotes prostate cancer proliferation and migration by restraining the ubiquitin-dependent degradation of LRP5. [Abstract]2025 Jul 25;44(1):218. PMID: 40713830
EPZ015666 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 25;44(1):218. [Abstract]
The DMA inhibitor EPZ015666 (10 µM) reduced the activity of Fluc in circSPIRE1 IRES transfected cells, but had no effect on Rluc.
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J Exp Clin Cancer Res
MYC up-regulation confers vulnerability to dual inhibition of CDK12 and CDK13 in high-risk Group 3 medulloblastoma. [Abstract]2023 Aug 21;42(1):214. PMID: 37599362 -
J Exp Clin Cancer Res
2022 Oct 5;41(1):293. PMID: 36199122 -
J Exp Clin Cancer Res
The PRMT5-LSD1 axis confers Slug dual transcriptional activities and promotes breast cancer progression. [Abstract]2022 Jun 2;41(1):191. PMID: 35655230
EPZ015666 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2022 Jun 2;41(1):191. [Abstract]
Changes in cell viability after treatment with 40 μM FKA, two PRMT5 inhibitors EPZ015666 (22 nM), and the first-line chemotherapy drug BC. Combined treatment with FKA or PRMT5 inhibitors and GC showed a synergistic effect on cell viability of T24 cells (left panel) and UMUC3 cells (right panel).
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Sci Adv
2024 Jun 7;10(23):eadm9589. PMID: 38838142
EPZ015666 purchased from MedChemExpress. Usage Cited in: Sci Adv. 2024 Jun 7;10(23):eadm9589. [Abstract]
CXCL10-HiBiT expression from CXCL10-HiBiT knock-in MCF10A cells treated with DMSO, HU (1 mM), HU (1 mM) + GSK591 (1 μM), and HU (1 mM) + EPZ015666 (1 μM) for 48 hours.
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Cancer Lett
Inhibition of PRMT5 moderately suppresses prostate cancer growth in vivo but enhances its response to immunotherapy. [Abstract]2024 Aug 30:217214. PMID: 39218291 -
Cell Commun Signal
2025 Mar 8;23(1):126. PMID: 40057764 -
Acta Pharmacol Sin
Adriamycin induces cardiac fibrosis in mice via PRMT5-mediated cardiac fibroblast activation. [Abstract]2023 Mar;44(3):573-583. PMID: 36056082 -
J Med Chem
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death. [Abstract]2024 Sep 12;67(17):15098-15117. PMID: 39145486 -
J Mol Cell Biol
Methylation of MATCAP by PRMT5 regulates microtubule detyrosination to ensure mitotic fidelity. [Abstract]2026 Mar 11:mjag008. PMID: 41811993 -
J Biol Chem
Prmt5 promotes ciliated cell specification of airway epithelial progenitors via transcriptional inhibition of Tp63. [Abstract]2023 Aug;299(8):104964. PMID: 37364687 -
J Biol Chem
Protein arginine methyltransferase 5 is essential for oncogene product EWSR1-ATF1-mediated gene transcription in clear cell sarcoma. [Abstract]2022 Oct;298(10):102434. PMID: 36041632 -
J Biol Chem
Extracellular 5'-methylthioadenosine inhibits intracellular symmetric dimethylarginine protein methylation of FUSE-binding proteins. [Abstract]2022 Sep;298(9):102367. PMID: 35963436 -
J Proteome Res
ETD-Based Proteomic Profiling Improves Arginine Methylation Identification and Reveals Novel PRMT5 Substrates. [Abstract]2024 Mar 1;23(3):1014-1027. PMID: 38272855 -
PLoS One
Asymmetric and symmetric protein arginine methylation in methionine-addicted human cancer cells. [Abstract]2023 Dec 22;18(12):e0296291. PMID: 38134182 -
Biomed Res Int
Protein Arginine Methyltransferase 5 Promotes the Migration of AML Cells by Regulating the Expression of Leukocyte Immunoglobulin-Like Receptor B4. [Abstract]2021 Oct 19;2021:7329072. PMID: 34712735 -
Exp Ther Med
Protein arginine methyltransferase 5 mediates THP-1-derived macrophage activation dependent on NF-κB in endometriosis. [Abstract]2021 Sep;22(3):1003. PMID: 34345285 -
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Solvant et solubilité
DMSO : 100 mg/mL (260.80 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (6.52 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 (6.52 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.
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.
Protocole
Cultured cells in linear/log-phase growth are split to a seeding density of 2×105 cells/mL in 2-20 mL of media, depending on the yield required at the end of the growth period. Compound is diluted in DMSO and added to each culture vessel with a final DMSO concentration of 0.2%. Cells are allowed to grow for 96 h undisturbed. At the conclusion of each treatment period, cells are harvested by centrifugation (5 min, 1,200 rpm), and cell pellets are rinsed once with PBS before being frozen on dry ice pending further processing. Long-term proliferation assays are performed on all MCL lines, with slight adjustments to initial seeding densities, depending on growth characteristics for each cell line. All assays are carried out for 12 d[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Male CD-1 mice (25-40 g; n=6, with 3 per time point) are treated with a single dose of EPZ015666 (GSK3235025) at 2 mg/kg by intravenous tail-vein injection and 10 mg/kg by oral gavage administration, with both doses formulated in 20% N-N-dimethylacetamide in water. Animals are fasted overnight and weighed before dose administration on the day of dosing. Approximately 30 μL of blood are taken from animals by submandibular or retro-orbital bleeding at pre-specified time intervals (seven time points). For the last time point (24 h), samples are collected via cardiac puncture while the animals are under anesthesia (70% CO2:30% O2). Blood samples are transferred into K2-EDTA tubes and placed on wet ice before centrifugation at 4°C (3,000g, 15 min) to obtain plasma within 30 min after sample collection. Plasma samples are stored at −70±10°C before protein precipitation and LC-MS/MS analysis. We constructed standard calibration curves by analyzing a series of control plasma aliquots containing 100 ng/mL labetalol as an internal standard and 1-3,000 ng/mL EPZ015666 (GSK3235025). Four levels of quality control are also included in the analysis (3-2,400 ng/mL EPZ015666 (GSK3235025)). Data are analyzed using Phoenix WinNonlin 6.2.1.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chan-Penebre E, et al. A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models. Nat Chem Biol. 2015 Jun;11(6):432-7. [Content Brief]
[2]. Kryukov GV, et al. MTAP deletion confers enhanced dependency on the PRMT5 arginine methyltransferase in cancer cells. Science. 2016 Mar 11;351(6278):1214-8. [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, 2 years; -20°C, 1 year. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6080 mL | 13.0398 mL | 26.0797 mL | 65.1992 mL |
| 5 mM | 0.5216 mL | 2.6080 mL | 5.2159 mL | 13.0398 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6080 mL | 6.5199 mL | |
| 15 mM | 0.1739 mL | 0.8693 mL | 1.7386 mL | 4.3466 mL | |
| 20 mM | 0.1304 mL | 0.6520 mL | 1.3040 mL | 3.2600 mL | |
| 25 mM | 0.1043 mL | 0.5216 mL | 1.0432 mL | 2.6080 mL | |
| 30 mM | 0.0869 mL | 0.4347 mL | 0.8693 mL | 2.1733 mL | |
| 40 mM | 0.0652 mL | 0.3260 mL | 0.6520 mL | 1.6300 mL | |
| 50 mM | 0.0522 mL | 0.2608 mL | 0.5216 mL | 1.3040 mL | |
| 60 mM | 0.0435 mL | 0.2173 mL | 0.4347 mL | 1.0867 mL | |
| 80 mM | 0.0326 mL | 0.1630 mL | 0.3260 mL | 0.8150 mL | |
| 100 mM | 0.0261 mL | 0.1304 mL | 0.2608 mL | 0.6520 mL |