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EPZ015666

Catalog No. T6076 CAS 1616391-65-1

Synonyms: GSK3235025

EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

EPZ015666, CAS 1616391-65-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 42.00
2 mg	In stock	$ 56.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 126.00
50 mg	In stock	$ 369.00
100 mg	In stock	$ 531.00
1 mL * 10 mM (in DMSO)	In stock	$ 93.00

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Purity: 99.92%

Purity: 99.4%

Purity: 99.29%

Purity: 98.60%

Purity: 98.37%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ015666 (GSK3235025) is an orally available inhibitor of PRMT5 enzymatic activity.
Targets&IC50	PRMT5:5 nM(Ki)
In vitro	Orally administered at a dosage of 200 mg/kg, EPZ015666 exhibits potent antitumor activity in the MCL xenograft animal model.
In vivo	EPZ015666 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.
Kinase Assay	EPZ015666 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].
Cell Research	EPZ015666 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].

Synonyms	GSK3235025
Molecular Weight	383.44
Formula	C20H25N5O3
CAS No.	1616391-65-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 56 mg/mL (146 mM)

Ethanol: 45 mg/mL (117.4 mM)

References and Literature

1. Penebre et al. Epizyme, Inc.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Highly Selective Inhibitor Library Anti-COVID-19 Compound Library Reprogramming Compound Library Hematonosis Compound Library Bioactive Compound Library Stem Cell Differentiation Compound Library Anti-Cancer Compound Library Target-Focused Phenotypic Screening Library

Related Products

Related compounds with same targets

GSK3368715 dihydrochloride EED226 PRMT5-IN-25 EPZ031686 EZM0414 EPZ011989 Chaetocin BRD0639

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

EPZ015666 1616391-65-1 Chromatin/Epigenetic Histone Methyltransferase inhibit Inhibitor GSK-3235025 EPZ 015666 EPZ-015666 GSK 3235025 GSK3235025 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.