Table 1: Differential scanning fluorimetry and cytotoxicity results for pre-miR-21 stability modulating compounds.
PubChem CID # is the compound’s identifier (https://pubchem.ncbi.nlm.nih.gov/). The ΔTm MAX was calculated by taking the melting temperature shift difference of pre-miR-21 treated with the compound vs untreated. aThe apparent Kd (Kdapp) was measured by direct binding assay using intrinsic fluorescence max 545/580 nm. bGI50 was determined using the XTT cell viability assay. Calculations were performed using the non-linear regression fit (Sigmoidal, 4PL) function in GraphPad Prism. cNormal colon cells used were ATCC CRL-1790. d1,5-bis[3-(2-hydroxyethylamino)propylamino]anthracene-9,10-dione hydrochloride. All experiments were repeated in triplicate.
| Compound number | PubChem CID | Short Name | ΔTm MAX (°C) | aKd (μM)app | GI50 (μM) HCT-116b | GI50 (μM) normal colonc |
|---|---|---|---|---|---|---|
| 1 | 54601748 | bPGN | +3.1 | 0.41 ± 0.04 | 0.035 ± 0.003 | ≥ 10 |
| 2 | 16681698 | Obatoclax | +3.2 | 0.09 ± 0.02 | 0.10 ± 0.01 | ≥ 10 |
| 3 | 5351169 | Prodigiosin | +7.0 | 0.16 ± 0.06 | 0.24 ± 0.04 | ≥ 10 |
| 4 | 5701988 | Aklavin | −17.1 | nd | 0.57 ± 0.06 | 1.7 ± 0.4 |
| 5 | 301935 | Trigilletine | +5.48 | nd | 3.5 ± 0.5 | 1.0 ± 0.2 |
| 6 | 5351330 | Anthraquinoned | +8.70 | nd | 3.2 ± 0.6 | 1.1 ± 0.8 |
| 7 | 5351224 | Lobinaline | −14.0 | nd | > 10 | > 10 |
| 8 | 5458561 | Prumycin | +8.41 | nd | > 10 | 5.1 ± 0.1 |
| 9 | 821347 | Dehydronuciferin | −15.7 | nd | > 10 | > 10 |
| 10 | 3385 | 5-FU | nd | nd | 0.72 ± 0.02 | 2.0 ± 0.2 |