Home Epigenetics Histone Methyltransferase inhibitor - PRMT inhibitor EPZ020411 2HCl For research use only.

EPZ020411 2HCl

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

EPZ020411 2HCl Chemical Structure

EPZ020411 2HCl Chemical Structure

CAS No. 2070015-25-5

Purity & Quality Control

EPZ020411 2HCl Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293F Function assay 30 mins Inhibition of FLAG and hexa-histidine tagged full-length human PRMT6 expressed in HEK293F cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix, IC50=0.01μM 26101569
insect cells Function assay 30 mins Inhibition of N-terminal GST tagged full-length human PRMT1 expressed in high five insect cells pre-incubated for 30 mins before addition of a [3H]SAM and peptide mix, IC50=0.119μM 26101569
A375 Function assay 0.01 to 20 uM 48 hrs Inhibition of his-tagged PRMT6 (unknown origin) expressed in human A375 cells assessed as reduction in H3R2 methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method, IC50=0.637μM 26101569
A375 Function assay 0.01 to 20 uM 48 hrs Inhibition of PRMT1 in human A375 cells assessed as effect on monomethyl R*GG motif methylation at 0.01 to 20 uM incubated for 48 hrs by Western blot method, IC50=7.1μM 26101569
Sf9 Function assay Non-competitive inhibition of N-terminal hexa-His tagged human PRMT6 expressed in Sf9 cells using 24 residues of biotin labelled histone4 substrate and tritiated 3H-S-adenosylmethionine by scintillation proximity assay 26824386
Click to View More Cell Line Experimental Data

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
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Sprague-Dawley rats
Dosages 1 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 515.52 Formula

C25H40Cl2N4O3
CAS No. 2070015-25-5 SDF Download EPZ020411 2HCl SDF
Smiles CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (193.97 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy EPZ020411 2HCl | EPZ020411 2HCl supplier | purchase EPZ020411 2HCl | EPZ020411 2HCl cost | EPZ020411 2HCl manufacturer | order EPZ020411 2HCl | EPZ020411 2HCl distributor