EPZ020411 2HCl

Catalog No.S7820

EPZ020411 2HCl Chemical Structure

Molecular Weight(MW): 515.52

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

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description EPZ020411 is a potent and selective small molecule PRMT6 inhibitor with an IC50 of 10 nM.
Targets
PRMT6 [1]
(Cell-free assay)
PRMT1 [1]
(Cell-free assay)
PRMT8 [1]
(Cell-free assay)
10 nM 119 nM 223 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). In biochemical assays EPZ020411 is over 100-fold selective for PRMT6/8/1 compared to other histone methyltransferases including four arginine methyltransferases (PRMT3, PRMT4, PRMT5, and PRMT7). The compound shows poor permeability in the parallel artificial membrane permeation assay[1].

In vivo EPZ020411 shows good bioavailability following subcutaneous dosing in rats making it a suitable tool for in vivo studies. Male Sprague-Dawley rats administered a single dose of EPZ020411 at 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. Following 5 mg/kg s.c. dosing, a good bioavailability of 65.6 ± 4.3% is observed, leading to EPZ020411 unbound blood concentration remaining above the PRMT6 biochemical IC50 value for more than 12 h[1].

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: A375 cells
  • Concentrations: 0-20 μM
  • Incubation Time: 48 h
  • Method: A375 (CRL-1619) cells are cultured in DMEM plus 10% (vol/vol) FBS. PRMT6 is cloned into BamHI and EcoRI sites of a pcDNA4 HisMAX_A plasmid. Transfection of his-tagged PRMT6 or vector control is carried out using Lipofectamine LTX and Plus reagent according to procedures recommended by the manufacturer. Cells are seeded at 200,000 cells/well in 6-well plates. The following day, the cells are concurrently transfected and treated with compound in 0.25% DMSO. Cells are incubated in the presence of increasing concentrations of compound up to 20 μM. Cell pellets are collected after 48 hours of compound treatment.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Sprague-Dawley rats
  • Formulation: saline, pH 6.5
  • Dosages: 1 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (193.97 mM)
Ethanol 100 mg/mL (193.97 mM)
Water 81 mg/mL (157.12 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 515.52
Formula

C25H40Cl2N4O3

CAS No. 1700663-41-7(free base)
Storage powder
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID