Table 2. Performance of 16 hits and erbstatin analog in the Alamar Blue viability assay.
Summary assessment of the 16 hits and the erbstatin analog effects on the viability of A549-EGFRB, A549, H2030, H3255 and HCC4011 cell lines. The reported IC50 values ±standard deviation were calculated based on dose response studies for each confirmed hit using the Alamar Blue viability assay as described under Materials and Methods.
| Alamar Blue viability assay IC50 (μM) | ||||||
|---|---|---|---|---|---|---|
| Compound name | Molecular target | A549 | H2030 | H3255 | HCC4011 | |
| Known EGFR inhibitors | BIBU 1361 | EGFR kinase | 3.7±0.8* | 3.1±0.7* | 0.020±0.004 | 0.035±0.003 |
| Tyrphostin AG 1478 | EGFR kinase | > 10 | > 10 | 0.049±0.001 | 0.033±0.007 | |
| PD 153035 | EGFR kinase | > 10 | > 10 | 0.072±0.012 | 0.048±0.012 | |
| Erlotinib | EGFR kinase | > 10 | > 10 | 0.045±0.005 | 0.048±0.006 | |
| Gefitinib | EGFR kinase | > 10 | > 10 | < 0.01 | 0.028±0.003 | |
| Lapatinib | EGFR kinase | > 10 | > 10* | 1.2±0.1 | 1.5±0.1 | |
| GW 2974 | EGFR kinase | > 10 | > 10 | 0.67±0.1 | 1.4±0.6* | |
| GW 583340 | EGFR kinase | > 10 | > 10 | 0.96±0.06 | 2.0±0.2 | |
| Erbstatin analog | EGFR kinase | > 10* | > 10* | > 10 | > 10* | |
| Other confirmed granule formation inhibitors | ZM-306416 | VEGFR kinase | > 10 | > 10 | 0.09±0.007 | 0.072±0.01 |
| Camptothecin | Topoisomerase I | 0.035±0.05 | 0.017±0.005 | 0.39±0.05 | 0.29±0.04 | |
| PKC 412 | Pan-kinase inhibitor | 0.34±0.03 | 2.0±1.7* | 1.9±0.2 | 2.3±0.6 | |
| Aminopurvalanol A | CDKs | > 10* | > 10* | > 10* | > 10* | |
| 17-DMAG | Hsp90 | < 0.01 | < 0.01 | 0.021±0.01* | 0.025±0.002* | |
| Confirmed granule formation activators | Flurandrenolide | Corticosteroid | > 10 | > 10 | > 10 | > 10 |
| Beclomethasone | Corticosteroid | > 10 | > 10 | > 10 | > 10 | |
| Ebastine | H1 receptor | > 10 | > 10 | > 10 | > 10 | |
*
partial inhibition: a clear upper asymptote was not reached at the highest concentrations tested, or the upper asymptote did not reach 100% inhibition.