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EPZ020411 hydrochloride

Catalog No. T22325 CAS 2070015-25-5

Synonyms: EPZ020411 HCl

EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.

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

EPZ020411 hydrochloride Chemical Structure

EPZ020411 hydrochloride, CAS 2070015-25-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 55.00
5 mg	In stock	$ 133.00
10 mg	In stock	$ 226.00
25 mg	In stock	$ 389.00
50 mg	In stock	$ 593.00
100 mg	In stock	$ 848.00
1 mL * 10 mM (in DMSO)	In stock	$ 148.00

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Purity: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.
Targets&IC50	PRMT8:223 nM, PRMT1:119 nM, PRMT6:10 nM
In vitro	Treatment with EPZ020411 results in a dose-dependent decrease in H3R2 methylation in A375 human melanoma cells exogenously overexpressing PRMT6(IC50=0.637±0.241 μM). EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including PRMT3, PRMT4, PRMT5, and PRMT7 in biochemical assays. The compound shows poor permeability in the parallel artificial membrane permeation assay[1].
In vivo	EPZ020411 shows good bioavailability following subcutaneous dosing in rats. Male Sprague-Dawley rats administered EPZ020411 at a single dose of 1 mg/kg by i.v. bolus show a moderate clearance (CL) of 19.7±1.0 mL/min/kg, with a volume of distribution at steady state (Vss) of 11.1±1.6 L/kg, translating to a mean terminal half-life (t1/2) of 8.54±1.43 h. A good bioavailability of 65.6 ± 4.3% is observed following 5 mg/kg s.c. dosing, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 for more than 12 h[1].
Cell Research	Cell lines: A375 cells. Concentrations: 0-20 μM. Incubation Time: 48 h. Method: A375 (CRL-1619) cells are cultured in DMEM with 10% (vol/vol) FBS. PRMT6 is cloned into EcoRI and BamHI sites of a pcDNA4 HisMAX_A plasmid. According to procedures recommended by the manufacturer, transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent . Cells are seeded at 200,000 cells/well in 6-well plates. The second day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence compound at 20 μM and collected after 48 hours treatment.
Animal Research	Animal Models: SD rats. Dosages: 1 mg/kg. Administration: i.v..

Synonyms	EPZ020411 HCl
Molecular Weight	479.05
Formula	C25H39ClN4O3
CAS No.	2070015-25-5

Storage

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

Solubility Information

H2O: 18.0 mg/mL (37.6 mM), Sonication and heating to 60℃ are recommended.

DMSO: 45.0 mg/mL (93.9 mM), Sonication is recommended.

References and Literature

1. Mitchell LH, et al. ACS Med Chem Lett. 2015, 6(6):655-9.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Histone Modification Compound Library Bioactive Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max Epigenetics Compound Library

Related Products

Related compounds with same targets

WDR5-0102 EPZ004777 GSK3368715 dihydrochloride EPZ020411 UNC3866 TFA(1872382-47-2 free base) GSK126 A-196 DCLX069

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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

EPZ020411 hydrochloride 2070015-25-5 Chromatin/Epigenetic Histone Methyltransferase EPZ 020411 Hydrochloride EPZ-020411 hydrochloride EPZ020411 HCl EPZ020411 Hydrochloride EPZ-020411 Hydrochloride inhibitor inhibit

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