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Table 1 In vitro and cellular IC50 of selected KDM inhibitors tested

From: Assessing histone demethylase inhibitors in cells: lessons learned

  KDM5A KDM5B KDM5C KDM5D KDM2A KDM3A KDM4A KDM4B KDM4C KDM6B
  IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM) IC50 (µM)
KDOAM-20 0.010 ± 0.0030 (6) 0.007 ± 0.0030 (12) 0.019 ± 0.0050 (10) 0.019 ± 0.0040 (6) 2.2 ± 0.37 (2) 1.2 ± 0.91 (4) 0.67 ± 0.23 (2) 0.099 (1) 0.19 ± 0.081 (6) 1.4 ± 0.45 (2)
In vitro
KDOAM-20 ND 20 ND ND ND ND ND ND ND ND
In cells
KDOAM-21 0.068 ± 0.010 (2) 0.094 ± 0.065 (6) 0.17 ± 0.073 (6) ND 19 ± 10 (2) 2.6 ± 1.3 (4) 11 ± 4.5 (2) 2.5 (1) 2.8 ± 1.3 (4) 11 ± 4.6 (2)
In vitro
KDOAM-21 4.8 0.7 3.1 4 NA NA 70 10* 17.9 NA
In cells
KDOAM-32 ND >10 (2) ND ND ND ND ND ND ND ND
In vitro
KDOAM-32 >100 >100 >100 >100 >100 >100 >100 >100 >100 >100
In cells
KDIPP15 0.040 ± 0.016 (2) 0.063 ± 0.028 (2) 0.26 ± 0.039 (2) 0.23 ± 0.039 (2) >100 (2) >100 (2) 3.9 ± 1.4 (3) 1.4 ± 0.47 (3) 5.1 ± 0.062 (4) >100 (2)
In vitro
KDIPP15 ND 20.7 ND ND ND ND ND ND ND ND
In cells
KDIPP51 (CCT364883) 0.015 ± 0.0041 (4) 0.014 ± 0.0046 (4) 0.024 ± 0.0044 (4) 0.024 ± 0.0038 (4) 8.6 ± 5.9 (2) 6.0 ± 3.9 (4) 0.126 ± 0.013 (2) 0.050 ± 0.0038 (2) 0.10 ± 0.031 (4) 44 ± 17 (3)
In vitro
KDIPP51 (CCT364883) ND 39.9# ND ND ND ND ND ND ND ND
In cells
CPI-455 0.16 ± 0.068 (2) 0.26 ± 0.064 (2) 7.8 ± 1.6 (2) ND 23 ± 3.5 (2) >100 (2) 31 (1) 44 (1) 11 ± 2.3 (2) >100 (2)
In vitro
CPI-455 ND 60 ND ND ND ND ND ND ND ND
iN cells
CCT365599 ND 0.023(2) 0.065(2) ND 12.9c 5.3c 0.102 ± 0.058 0.031 ± 0.012 ND 15% at 100 µMc
In vitroa
CCT365599 ND >50 ND ND ND ND 10 ND ND ND
In cells
CCT366293 ND >10c >10c ND ND ND >10 (2) >10 (2) ND ND
In vitroa           
CCT366293 ND >100 ND ND ND ND >100 ND ND ND
In cells
IOX1 ND 20.6 ± 9.0 (10) 30.4 ± 13.2 (13) ND 5 ± 3.8 (4) 0.2 ± 0.22 (30) 0.5 ± 0.4 (2) ND 3.5 ± 2.9 (16) 1.2 ± 1.3 (55)
In vitroa
IOX1 ND 62 ND ND ND ND ND ND ND ND
In cells
JIB-04 E ND 0.561 (1) 0.622 ± 0.05 (2) ND 1.2 ± 0.01 (3)d 0.65 ± 0.05 (3) ND ND 0.62 ± 0.02 (2) 1.04 ± 0.6 (4)
In vitroa
JIB-04 E ND 3 ND ND ND ND ND ND ND ND
In cells
JIB-04 Z ND 7.01 (1) >10 (3) ND ND >10 (3) ND ND >10 (2) >10 (4)
In vitro
JIB-04 Z ND >100 ND ND ND ND ND ND ND ND
In cells
  1. In vitro
  2. IC50 values ± SD (number of replicates) determined by the AlphaScreen assay
  3. aIn vitro biochemical profiling was previously reported [11]
  4. bBiochemical assay protocols as previously reported [11]. CCT366293 displays assay interference above 10 μM
  5. cResults are from a single determination
  6. dResults are determined by RapidFire under low iron condition (0.2 mM)
  7. In cells
  8. EC50 values were determined by IF assay
  9. Results are mean values of at least 3 independent experiments unless indicated otherwise
  10. * Results from 2 independent experiments
  11. #Highest concentration was excluded from calculation