Home Epigenetics Histone Methyltransferase inhibitor - EZH1/2 inhibitor EPZ011989 For research use only.

EPZ011989

EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.

EPZ011989 Chemical Structure

EPZ011989 Chemical Structure

CAS No. 2095432-26-9

Purity & Quality Control

EPZ011989 Related Products

Signaling Pathway

Histone Methyltransferase Signaling Pathways

Histone Methyltransferase Signaling Pathway

Biological Activity

Description EPZ011989 is a potent, selective, orally bioavailable EZH2 inhibitor with Ki of <3 nM.
Targets
EZH2 [1]
(Cell-free assay)		 EZH1 [1]
(Cell-free assay)
<3 nM(Ki) 103 nM
In vitro
In vitro EPZ011989 equipotently inhibits mutant and wild-type EZH2 with an inhibition constant (Ki) of <3 nM. EPZ011989 is also a specific EZH2 inhibitor with a >15-fold selectivity over EZH1 and >3000-fold selectivity relative to the Ki of 20 other histone methyltransferases (HMTs) tested. As evidenced by the human and rat liver microsomal turnover, EPZ011989 also exhibits metabolic stability. EPZ011989 reduces cellular H3K27 methylation in the Y641F, mutant-bearing human lymphoma cell line, WSU-DLCL2, with an IC50 below 100 nM[1]. EPZ011989 inhibits H3K27me3 in wild-type EZH2 AML cell lines (Kasumi-1, MOLM-13, and MV4-11) at a concentration of 0.625 μM after only four days of treatment. At these concentrations and this time point, no change in viability among these three cell lines is observed and only minimal proliferation inhibition in MV4-11 and MOLM-13 cells[2].
Cell Research Cell lines WSU-DLCL2 cells
Concentrations 0-10 μM
Incubation Time 0-11 days
Method

For assessment of cell proliferation and viability, exponentially growing cells are plated, in triplicate, in 96-well plates. Cells are incubated with increasing concentrations of EPZ011989. Viable cell number is determined every 3-4 days for up to 11 days using the Guava Viacount assay.
In Vivo
In vivo EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma. EPZ011989 is able to elicit robust methyl mark inhibition and antitumor activity[1].
Animal Research Animal Models SCID mice
Dosages 250 and 500 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 642.27 Formula

C35H51N5O4·HCl
CAS No. 2095432-26-9 SDF Download EPZ011989 SDF
Smiles CCN(C1CCC(CC1)N(C)CCOC)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C#CCN4CCOCC4.Cl
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 100 mg/mL

DMSO : 5 mg/mL ( (7.78 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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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