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Postion:Product Catalog >Biochemical Engineering>Inhibitors>Epigenetics>Histone Methyltransferase Inhibitors>EPZ015666
EPZ015666
  • EPZ015666

EPZ015666 NEW

Price $56 $85 $126
Package 2mg 5mg 10mg
Supply Ability: 10g
Update Time: 2026-06-02

Product Details

Product Name: EPZ015666 CAS No.: 1616391-65-1
Purity: 99.36% Supply Ability: 10g
Release date: 2026/06/02

Product Introduction

Bioactivity

NameEPZ015666
DescriptionEPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
Cell ResearchEPZ015666 is dissolved in DMSO and stored, and then diluted with appropriate medium (final DMSO 0.2%) before use[1]. 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].
Kinase AssayEPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. 3H-SAM is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 700 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 40 nM peptide (final assay concentrations for both). Reactions are incubated for 60 min and quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration). For the peptide competition, EPZ015666 is serially diluted threefold from 1,000 to 0.051 nM and spotted into a 384-well polypropylene V-bottom microplate. Peptide is serially diluted twofold in assay buffer for a seven-point dilution series with a top concentration of 480 nM (final assay concentration). Reactions are initiated by the addition of 4 nM enzyme and 75 nM 3H-SAM (final assay concentrations for both). Reactions are incubated for 60 min, and the reactions are quenched by the addition of 10 μL per well of 600 μM unlabeled SAM in assay buffer (final assay concentration)[1].
In vitroOrally administered at a dosage of 200 mg/kg, EPZ015666 exhibits potent antitumor activity in the MCL xenograft animal model.
In vivoEPZ015666 demonstrates effective cellular activity by blocking the symmetrical dimethylation of SmD3 and inhibiting the proliferation of MCL cell lines, with an IC50 range of 96-904 nM.
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility InformationDMSO : 245 mg/mL (638.95 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (26.08 mM), Solution.
Ethanol : 45 mg/mL (117.36 mM), Sonication is recommended.
10% DMSO+90% Saline : 10 mg/mL (26.08 mM), Solution.
KeywordsPRMT5 | Inhibitor | inhibit | HistoneMethyltransferase | Histone Methyltransferase | GSK-3235025 | GSK 3235025 | EPZ-015666 | EPZ015666 | EPZ 015666
Inhibitors RelatedMAK-683 hydrochloride | SNDX-5613 | Tazemetostat | Piribedil | XY1 | UNC 0631 | (Iso)-Flavokawain A | MAK683 | iso-Azalansta | AMI-1 free acid | MS37452 | MRTX-1719
Related Compound LibrariesHighly Selective Inhibitor Library | Methylation Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Stem Cell Differentiation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Preclinical Compound Library | Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library

Company Profile Introduction

Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers. TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.

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