EPZ020411 2HCl

Catalog No.S7820

For research use only.

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

EPZ020411 2HCl Chemical Structure

CAS No. 2070015-25-5

Selleck's EPZ020411 2HCl has been cited by 2 Publications

Purity & Quality Control

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].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293F NH7TZmxHfW6ldHnvckBie3OjeR?= NXrzZmk1OzBibXnudy=> MWDJcohq[mm2aX;uJI9nKE[OQVegZY5lKGineHGtbIl{fGmmaX7lJJRi\2enZDDmeYxtNWynbnf0bEBpfW2jbjDQVm1VPiCneIDy[ZN{\WRiaX6gTGVMOjl|RjDj[YxteyCycnWtbY5kfWKjdHXkJIZweiB|MDDtbY5{KGKnZn;y[UBi\GSrdHnvckBw\iCjIGuzTH1USU1iYX7kJJBmeHSrZHWgcYl5NCCLQ{WwQVAvODIQvF2= MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFyMUW2PUc,OjZzMEG1Olk9N2F-
insect cells M3XTN2Z2dmO2aX;uJIF{e2G7 NVLWdJc2OzBibXnudy=> Mn[5TY5pcWKrdHnvckBw\iCQLYTldo1qdmGuIFfTWEB1[WepZXSg[pVtdC2uZX7neIghcHWvYX6gVHJOXDFiZYjwdoV{e2WmIHnuJIhq\2hiZnn2[UBqdnOnY4SgZ4VtdHNicILlMYlv[3WkYYTl[EBnd3JiM{CgcYlveyCkZX\vdoUh[WSmaYTpc44hd2ZiYTDbN2heW0GPIHHu[EBx\XC2aXTlJI1qgCxiSVO1NF0xNjFzOd88US=> Ml;RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZzMEG1OlkoRjJ4MUCxOVY6RC:jPh?=
A375 M2TITmZ2dmO2aX;uJIF{e2G7 M4DHWlAvODFidH:gNlAhfU1? MlTKOFghcHK| NXzwWIFxUW6qaXLpeIlwdiCxZjDobZMufGGpZ3XkJHBTVVR4IDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJIh2dWGwIFGzO|Uh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKGmwIFizVlIhdWW2aInsZZRqd25iYYSgNE4xOSC2bzCyNEB2VSCrbnP1ZoF1\WRiZn;yJFQ5KGi{czDifUBY\XO2ZYLuJIJtd3RibXX0bI9lNCCLQ{WwQVAvPjN5zszN MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFyMUW2PUc,OjZzMEG1Olk9N2F-
A375 MorDSpVv[3Srb36gZZN{[Xl? M1npbVAvODFidH:gNlAhfU1? MYm0PEBpenN? NX3jWXpGUW6qaXLpeIlwdiCxZjDQVm1VOSCrbjDoeY1idiCDM{e1JINmdGy|IHHzd4V{e2WmIHHzJIVn\mWldDDvckBud26xbXX0bJltKFJsR1egcY91cWZibXX0bJlt[XSrb36gZZQhOC5yMTD0c{AzOCC3TTDpcoN2[mG2ZXSg[o9zKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgcYV1cG:mLDDJR|UxRTdwMd88US=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjFyMUW2PUc,OjZzMEG1Olk9N2F-
Sf9 MY\GeY5kfGmxbjDhd5NigQ>? MVLOc44u[2:vcHX0bZRqfmViaX7obYJqfGmxbjDv[kBPNXSncn3pcoFtKGineHGtTIl{KHSjZ3fl[EBpfW2jbjDQVm1VPiCneIDy[ZN{\WRiaX6gV4Y6KGOnbHzzJJV{cW6pIEK0JJJme2mmdXXzJI9nKGKrb4TpckBt[WKnbHzl[EBpcXO2b37lOEB{fWK|dILheIUh[W6mIITybZRq[XSnZDCzTE1UNWGmZX7vd5ltdWW2aHnvcolv\SCkeTDzZ4lvfGmubHH0bY9vKHC{b4jpcYl1gSCjc4PhfS=> NH;XfJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkiyOFM5Pid-Mk[4NlQ{QDZ:L3G+
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 (from reference)

Cell Research:[1]
  • 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.
Animal Research:[1]
  • Animal Models: Sprague-Dawley rats
  • Dosages: 1 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 515.52
Formula

C25H40Cl2N4O3

CAS No. 2070015-25-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNCCN(C)CC1=C(NN=C1)C2=CC=C(C=C2)OC3CC(C3)OCCC4CCOCC4.Cl

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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