Table 1.
Pharmacological inhibitors, their abbreviations, and their specificities
| Reagent | Tag | Endocytosis pathway blocked | Specificity | Reference(s) |
|---|---|---|---|---|
| PAK-1 inhibitor peptide | PAK-18 | Macropinocytosis | Autoinhibitory domain of PAK-1 | 88, 124, 125 |
| Inactive control peptide (PAK18-R192A) | PAK-NC | Control for PAK-18 | Inactive peptide that controls for nonspecific effects | |
| RacGEF inhibitor (NSC23766) | RAC-I | Macropinocytosis | Inhibits Rac-1 GDP/GTP exchange | 26, 85, 90 |
| p21-activated kinase inhibitor III | IPA-3 | Macropinocytosis | Prevents PAK-1 activation (irreversible) | 26, 66, 90 |
| 5-(N-Ethyl-N-isopropyl)amiloride | EIPA | Macropinocytosis | Inhibits Na+/H+ exchange | 38, 53, 88 |
| Cell-permeant 17β-hydroxy analog of wortmannin | HWT | Macropinocytosis | Irreversible PI3K inhibitor | 64, 66 |
| LY294002 | Macropinocytosis | Reversible PI3K inhibitor | 44, 71, 90 | |
| Cytochalasin D | CD | Macropinocytosis | Actin-depolymerizing agent | 40, 64, 94 |
| Latrunculin A | LA | Macropinocytosis and clathrin | Sequesters actin monomers | 31, 40, 64, 120 |
| Jasplakinolide | JP | Macropinocytosis and caveolin | Stabilizes actin polymers | 31, 64, 94 |
| Ammonium chloride | NH4Cl | All pH dependent | Blocks acidification of endosomes | 74 |
| Bafilomycin A1 | BAF | All pH dependent | Inhibits vacuolar H+-ATPase (irreversible) | 123 |
| Chlorpromazine | CPZ | Clathrin | Prevents clathrin-coated pit assembly at the cell surface | 11, 49, 72, 107 |
| Dynasore | DYN | Caveolin and clathrin | Blocks dynamin II | 40–42, 46, 51 |
| Okadaic acid | OA pre | Caveolin and clathrin | Removes cell surface caveolae and blocks CME | 5, 13, 59, 76, 77, 126 |
| Okadaic acid; cells treated for 1 h, postinfection | OA post | Enhances caveolin | Promotes CavME of bound cargo | 5, 76, 77, 126 |
| Phorbol 12-myristate 13-acetate | PMA | Caveolin | Decreases the level of caveolae at the cell surface | 2, 14, 102 |
| Nystatin + progesterone | Nys+Prog | Caveolin | Sequesters and blocks cholesterol | 2, 17, 21, 114 |