Table 1.

KD5170 inhibits both class I and class II HDAC isoforms

Recombinant human HDAC
CompoundHeLa
1
2
3
4
5
6
7
8
9
10
IC50 ± SE (μmol/L)
KD51700.045 ± 0.0070.020 ± 0.0042.06 ± 0.120.075 ± >0.010.026 ± 0.0030.95 ± 0.030.014 ± 0.0020.085 ± 0.0092.50 ± 0.340.15 ± 0.0050.018 ± 0.001
Compound 3 (disulfide)0.014 ± 0.0030.024 ± 0.0070.74 ± 0.080.014 ± 0.0030.023 ± 0.0020.36 ± 0.020.002 ± 0.00020.07 ± 0.0090.58 ± 0.040.092 ± 0.0080.015 ± 0.0009
TSA0.001 ± 00.012 ± 0.0030.020 ± 0.00050.010 ± 0.0050.022 ± 0.0060.016 ± 0.0030.0020 ± 00.081 ± 0.040.12 ± 0.010.080 ± 0.040.028 ± 0.01
  • NOTE: HDAC activity was determined indirectly by measuring the fluorescence generated by a deacetylated fluorogenic peptide product (Materials and Methods). Data presented represent mean ± SE. KD5170 and KLYP902195, n = 5 replicate assay runs for HeLa cell nuclear extract and HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC6, HDAC7, HDAC8, and HDAC10. HDAC9, n = 3. TSA, n = 2 for HeLa cell nuclear extract and all HDAC isoforms.