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

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


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In vivo
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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 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.

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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

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