1. Epigenetics
  2. Histone Methyltransferase
  3. EZH2-IN-4

EZH2-IN-4 

Cat. No.: HY-139150
Handling Instructions

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity.

For research use only. We do not sell to patients.

EZH2-IN-4 Chemical Structure

EZH2-IN-4 Chemical Structure

CAS No. : 2088132-99-2

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Description

EZH2-IN-4 is an orally active, potent EZH2 inhibitor with IC50s of 0.923 nM and 2.65 nM against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, respectively. EZH2-IN-4 has anti-cancer activity[1].

IC50 & Target[1]

WT 5-mer EZH2

0.923 nM (IC50)

mut 5-mer EZH2

2.65 nM (IC50)

In Vitro

EZH2-IN-4 (example 38) shows a cell H3K27me3 IC50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1].
EZH2-IN-4 shows an IC50 of 10.1 nM in Plate Kj«pas-422 cells[1].
EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC50s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC50>20 μM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1].
EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

511.72

Formula

C₂₉H₄₁N₃O₃S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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EZH2-IN-4
Cat. No.:
HY-139150
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