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Table 1 IC50 values, or percentage of inhibition at 200 μM, of MC4040 and MC4041 against a panel of methyltransferases

From: RETRACTED ARTICLE: Dissecting the role of novel EZH2 inhibitors in primary glioblastoma cell cultures: effects on proliferation, epithelial-mesenchymal transition, migration, and on the pro-inflammatory phenotype

Compound

IC50, μMa or % inhibition at 200 μM

EZH2

EZH1

G9a

PRMT1

DNMT1

MC4040

4.06

42.7

NAb

NA

NA

MC4041

1.06

10.6

NA

11.9%

NA

SAH

34.7

    

GSK126

0.009

    

TAZc

<0.005

    
  1. aPerformed in a 10-dose IC50 mode with 2-fold serial dilution starting from 200 μM. b NA, not active. c TAZ, tazemetostat
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Clinical Epigenetics

ISSN: 1868-7083

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