Table 2 IC50 values for EI1, EPZ-6438 and compound 3 against PRC2WT, PRC2Y111L, PRC2Y641N and PRC2Y641N/Y661D

From: Development of secondary mutations in wild-type and mutant EZH2 alleles cooperates to confer resistance to EZH2 inhibitors

Inhibitor

Substrate

WT (μ M)

Y111L (μ M)

Y641N (μ M)

Y641N/Y6661D (μ M)

EI1

Me0

0.2±0.03

>25

(−)

(−)

 

Me1

0.06±0.0

>25

0.1±0.03

>25

 

Me2

(−)

(−)

0.2±0.05

>25

EPZ-6438

Me0

0.2±0.04

11.5±4.3

(−)

(−)

 

Me1

0.06±0.01

9.2±2.7

0.1±0.03

2.8±1.1

 

Me2

(−)

(−)

0.1±0.04

3.4±0.8

Compound 3

Me0

2.02±0.4

>25

(−)

(−)

 

Me1

0.9±0.2

>25

6.1±0.8

>25

 

Me2

(−)

(−)

8.7±1.1

>25

  1. Abbreviation: WT, wild type.
  2. The biochemical reaction was carried out with [SAM] at 20 μM. The assay was carried out with [SAM] of 20 μM. When indicated with (-), those conditions were not tested due to low basal activity.
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