Table 2.
Combination of PAK1 inhibition with pharmarray small-molecule panel
| Compound | Single-agent EC50 (mM) | Combination PAKi EC50 (mM) | Fold change in EC50 | Trade name | Mechanism of action and/or approved use |
| BV6 | 20 | 0.35 | 57.54 | n/a | Antagonist of inhibitor of apoptosis (IAP) proteins |
| Erlotinib | 20 | 1.56 | 15.02 | Tarceva | Epidermal growth factor receptor (EGFR) inhibitor for NSCLC |
| Gefitinib | 20 | 3.3 | 12.8 | Iressa | EGFR kinase inhibitor |
| G-416 | 20 | 1.67 | 12 | n/a | Antagonist of IAP proteins |
| U0126 | 19.46 | 2.3 | 8.45 | n/a | Inhibitor of MAPK/ERK kinase-1/2 (MEK1/2) |
| Lapatinib | 6.31 | 0.86 | 7.34 | Tykerb | EGFR/HER2 inhibitor used for HER2-positive breast cancer |
| Dasatinib | 8.29 | 1.53 | 5.43 | Sprycel | Dual BCR/ABL and Src family kinase inhibitor for CML |
| Altretamine | 20 | 3.94 | 5.07 | Hexalen | Alkylating chemotherapy used for refractory ovarian cancer |
| Oxaliplatin | 10.5 | 2.48 | 4.23 | Eloxatin | Platinum-based chemotherapy used for colorectal cancer |
| ZD6474 | 20 | 6.88 | 2.91 | Vandetanib | VEGF and EGF inhibitor in clinical development |
| Akt VIII | 3.21 | 2.03 | 1.58 | n/a | Akt-1/2 kinase inhibitor |