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Table 1 RT-PCR data for a single dose of a panel of HKMT inhibitor compounds

From: Dual EZH2 and EHMT2 histone methyltransferase inhibition increases biological efficacy in breast cancer cells

Entry

 

Compound

KRT17

FBXO32

JMJD3

EZH2

1

Hit

HKMTI-1-005

4.05

3.65

3.12

0.63

2

Hit

HKMTI-1-022

4.28

29.4

11.56

0.21

3

Hit

HKMTI-1-11

6.95

33.25

6.25

0.22

4

G9ai

BIX01294

1.06

3.34

2.7

0.87

5

G9ai

UNC0638a

1.1

5.5

3.4

0.4

6

EZH2i

GSK343

0.9

1.2

1.0

1.0

7

Negative

HKMTI-1-002

0.66

1.12

1.57

0.86

8

Negative

HKMTI-1-012

1.32

1.06

0.9

1.38

9

Negative

HKMTI-1-013

0.78

0.93

0.87

0.13

  1. RNA levels for target genes are normalised against the housekeeping gene GAPDH, and shown is the fold increase compared to the mock treated sample
  2. aUNC0638 treatment at 7.5 μM, all other compounds given at 10 μM