Table 1.
Positive hits from the Cayman Epigenetics Screening Library. These compounds reduced RFP by at least 50% at 24 hpi - the percentage values indicate the RFP levels in cells treated with 1 μM drug relative to vehicle-treated cells (100% RFP) in the screen.
| Compound | % RFPa | Mode of action |
|---|---|---|
| 1) Chaetocinb | 10 | Methyltransferase inhibitor |
| 2) Apicidinb | 12 | HDAC inhibitor |
| 3) HC Toxinb | 13 | HDAC inhibitor |
| 4) Panobinostatb | 14 | HDAC inhibitor |
| 5) Givinostat | 17 | HDAC inhibitor |
| 6) Oxamflatin | 17 | HDAC inhibitor |
| 7) Gemcitabineb | 18 | DNA synthesis inhibitor |
| 8) Trifluoroacetate salt | 29 | HDAC inhibitor |
| 9) Pracinostat | 20 | HDAC inhibitor |
| 10) TSA | 22 | HDAC inhibitor |
| 11) Lestaurtinib | 22 | Tyrosine kinase inhibitor |
| 12) Decitabine | 25 | DNMT-1 inhibitor |
| 12) LAQ824b | 32 | HDAC inhibitor |
| 14) CAY10603 | 34 | HDAC inhibitor |
| 15) CUDC-101 | 37 | Multi-targeted inhibitor of HDACs, EGFR, HER2 |
| 16) M344 | 41 | HDAC inhibitor |
| 17) 4-iodo-SAHA | 45 | HDAC inhibitor |
| 18) CBHA | 47 | HDAC inhibitor |
| 19) Scriptaid | 49 | HDAC inhibitor |
Values represent the mean of three experimental replicates. The CV for all compounds was <35%, with the exception of CUDC-101 (61%) and LAQ824 (111%).
These compounds were also identified as positive hits when the screen was conducted with all compounds at 0.25 μM. The RFP percentage for chaetocin, apicidin, HC toxin, panobinostat, gemcitabine and LAQ824 were 34%, 42%, 35%, 32%, 44% and 32%, respectively.