Table 5. Summary of Cell-Based Testing of Novel ADAM17 Inhibitors for Suppression of Shedding of Cell-Surface Proteinsa.
| target ID | cell line | [C] tested (μM) | 16 | 17 | 18 | 19 | 20 | 21 |
|---|---|---|---|---|---|---|---|---|
| TNFα | THP1 | 25 | 57 | 43 | 36 | 60 | 44 | 0 |
| PTK7 | HT1080 | 25–100 | 0 | 25–50 | 0 | 0 | NT | NT |
| PTK7 | SW480 | 25–100 | 0 | 0–82 | 0 | 0 | NT | NT |
| DDR1 | HCC1806 | 10–40 | NT | 59–81 | NT | NT | NT | NT |
| IL-8 | HTSMC | 10 | 62 | 36 | 18 | NT | 62 | NT |
| FKN | HTSMC | 10 | 0 | 0 | 0 | NT | 0 | NT |
| CXCL16 | HTSMC | 10 | 0 | 0 | 0 | NT | 0 | NT |
| Heregulin | A549 | 40 | 0 | 100 | 0 | 28 | 0 | 34 |
| TGFα | A549 | 40 | 0 | 0 | 0 | 0 | 0 | 0 |
| BTC | A549 | 40 | 0 | 0 | 0 | NT | 0 | 0 |
| Notchb | SKMEL-28 | 25 | NT | 0 | NT | NT | NT | NT |
| Neprilysin63 | Ea.hy926 | 15 | NT | NT | 62 | 38 | NT | NT |
a
Data reported as inhibition, %. NT: not tested.
b
Personal communication from Dr. Kaushik (Kansas University Medical Center).