Summary of all HDAC IC50 values
Molecule name | HDAC protein members IC50 (mol/L) | ||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|
1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | 10 | 11 | |
Vorinostat | 0.06 | 0.042 | 0.036 | 0.02 | 0.036 | 0.029 | 0.129 | 0.173 | 0.049 | 0.060 | 0.031 |
Tucidinostat | 0.1 | 0.2 | 0.1 | > 10 | > 10 | > 10 | > 10 | 0.7 | > 10 | 0.1 | 0.4 |
Romidepsin | 0.001 | 0.001 | 0.001 | 647 | > 1 | 226 | > 1 | > 1 | > 1 | 0.001 | 0.0003 |
Panobinostat | 0.003 | 0.002 | 0.002 | 0.001 | 0.001 | 0.001 | 0.002 | 0.022 | 0.001 | 0.031 | 0.004 |
Belinostat | 0.026 | 0.022 | 0.019 | 0.015 | 0.025 | 0.010 | 0.051 | 0.022 | 0.024 | 0.059 | 0.027 |
Trichostatin A | 0.00068 | 0.0027 | 0.0004 | > 1 | 0.776 | 0.00095 | 0.482 | 0.207 | > 1 | 0.0016 | > 1 |
Quisinostat | 0.00062 | 0.002 | 0.00048 | 0.0046 | 0.006 | 0.0399 | 0.004 | 0.0024 | 0.0067 | 0.002 | > 1 |
Pracinostat* | 0.028 | 0.027 | 0.019 | 0.016 | 0.021 | 0.247 | 0.107 | 0.048 | 0.024 | 0.023 | 0.043 |
Abexinostat* | 0.007 | 0.019 | 0.0082 | - | - | 0.017 | - | 0.028 | - | 0.024 | - |
Fimepinostat | 0.0017 | 0.005 | 0.0018 | 0.409 | 0.647 | 0.027 | 0.426 | 0.191 | 0.554 | 0.0028 | 0.0054 |
HDAC-IN-30 | 0.0134 | 0.028 | 0.0092 | - | - | 0.0427 | - | 0.131 | - | - | - |
MMH409 | - | - | - | - | - | - | - | 0.0234 | - | - | - |
PCI-34051 | 4 | > 50 | > 50 | > 50 | - | - | 2.9 | 0.010 | - | 13 | - |
Chidamide | 0.095 | 0.160 | 0.067 | > 10 | > 10 | > 10 | > 10 | 0.733 | > 10 | 0.078 | 0.432 |
Tacdeinaline | 0.900 | 0.900 | 1.2 | - | - | - | - | > 20 | - | - | - |
Entinostat | 0.243 | 0.453 | 0.248 | > 10 | > 10 | > 10 | > 10 | > 10 | > 10 | > 10 | - |
BRD-6929 | 0.001 | 0.008 | 0.458 | > 10 | > 10 | > 10 | > 10 | > 10 | > 10 | 3.4 | - |
Mocetinostat | 0.150 | 0.290 | 1.6 | > 10 | > 10 | > 10 | > 10 | > 10 | - | - | 0.590 |
ACY-957 | 0.007 | 0.018 | 1.3 | NI | NI | NI | NI | NI | NI | - | - |
Compound 1 | 0.006 | 0.190 | 27.7 | > 50 | - | > 50 | - | 31.7 | - | - | - |
BRD-4884 | 0.029 | 0.062 | 1.09 | - | - | - | - | - | - | - | - |
BRD-3349 | 0.011 | 0.049 | 2.78 | - | - | - | - | - | - | - | - |
RGFP109 | 0.300 | 1.28 | 0.063 | > 180 | > 180 | >180 | > 180 | 10.7 | - | - | - |
RGFP136 | 5.2 | 3 | 0.400 | > 180 | > 180 | > 180 | > 180 | 13.2 | - | - | - |
RGFP966 | 5.6 | 9.7 | 0.210 | - | - | - | - | >100 | - | - | - |
BRD-3308 | 1.26 | 1.34 | 0.054 | > 33 | > 33 | > 33 | > 33 | > 33 | > 33 | - | - |
BG45 | 2 | 2.2 | 0.289 | - | - | > 20 | - | - | - | - | - |
T326 | > 100 | - | 0.260 | >100 | - | > 100 | - | >100 | - | - | - |
Compound 2 | > 30 | >30 | 0.120 | - | - | > 30 | - | > 30 | - | - | - |
Compound 3 | 0.080 | 0.110 | 0.006 | > 100 | > 100 | > 100 | > 100 | 0.0252 | > 100 | > 2 | > 4 |
UF010 | 0.500 | 0.100 | 0.060 | > 100 | > 100 | 9.1 | > 100 | 1.5 | > 100 | 15.3 | 44.5 |
SR-4370 | 0.130 | 0.580 | 0.006 | - | - | 2.3 | - | 3.7 | - | - | - |
Compound 4 | 0.0118 | 0.0955 | 0.00095 | - | - | - | - | - | - | - | - |
Compound 5 | 0.0633 | 0.287 | 0.0085 | - | - | > 100 | - | - | - | - | - |
Compound 6 | 0.00954 | 0.028 | 0.00141 | - | - | > 100 | - | - | - | - | - |
Compound 7 | 0.00469 | 0.046 | 0.00028 | > 10 | > 10 | > 50 | > 10 | > 1.75 | > 10 | - | - |
Largazole* | 0.020 | 0.021 | 0.048 | - | - | > 1 | - | - | - | - | - |
Largazole thiol* | 0.00007 | 0.00007 | 0.000017 | - | - | 0.025 | - | - | - | - | - |
Psammaplin A* | 0.045 | - | - | - | - | 2.8 | - | - | - | - | - |
Psammaplin A thiol | 0.0009 | - | - | - | - | 0.360 | - | - | - | - | - |
Compound 8 | 20 | 31 | 0.029 | > 40 | > 40 | > 45 | > 40 | > 45 | > 45 | 10 | 2 |
Compound 9 | 0.0097 | 0.029 | 0.0076 | - | - | 9 | - | > 45 | - | - | - |
Compound 10 | 0.040 | 0.061 | 0.0093 | - | - | > 45 | - | > 45 | - | - | - |
Compound 11 | 0.013 | 0.018 | 0.012 | - | - | 9 | - | > 45 | - | - | - |
Compound 12 | 0.0001 | 0.00047 | 0.000087 | - | - | > 45 | - | 0.016 | - | - | - |
Compound 13 | - | 0.500 | - | - | - | - | - | - | - | - | - |
Structures are present in the tables corresponding to the molecules [9, 14, 19, 21–23, 42, 43, 45–50, 52, 56, 57, 60–68, 71, 73, 74, 78, 80–91]. *: Ki value reported in place of an IC50; NI: no inhibition observed; -: not applicable
DIA, EDdA, and PTG: Conceptualization. DIA, NHP, and LSH: Investigation, Data collection. DIA: Writing—original draft. DIA, EDdA, OHK, RM, NHP, LSH, and PTG: Writing—review & editing. DIA, EDdA, OHK, RM, and PTG: Validation. DIA and PTG: Supervision. All authors read and approved the submitted version.
The authors declare that they have no conflicts of interest.
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© The Author(s) 2023.