Table 3.
Pharmacological and physical inhibitors of cellular uptake process.
| Inhibitor | Mechanism | Working condition | Ref. |
|---|---|---|---|
| Low temperature | Inhibit energy-dependent endocytosis | 4°C | [17] |
| Hypertonic medium | Inhibit clathrin-dependent endocytosis (Dissociate clathrin lattice) |
0.2–0.45 M sucrose | [17, 50] |
| Potassium depletion | Inhibit clathrin-dependent endocytosis (Dissociate clathrin lattice) |
50% DMEM w/1 mM ouabain | [50] |
| Fusicoccin | Endocytosis inhibitor (H+-ATPase activator) |
10 μM | [51] |
| Valinomycin/nigericin | Inhibit energy-dependent endocytosis (Na+/K+ ATPase modulator; K+ selective ionophore) |
2 μM | [52, 53] |
| Sodium azide/sodium fluoride/antimycin A | Inhibit energy-dependent endocytosis (All metabolic inhibitors) |
(0.15%/15 mM/2 μg/mL) | [17] |
| Okadaic acid | Endocytosis and autophagy inhibitor | 1.5 μM | [4, 26] |
| Nocodazole | Inhibit clathrin-dependent endocytosis (Cause microtubule depolymerization) |
10–25 μM | [17, 54] |
| Latrunculin A | Inhibit micropinocytosis (F-actin depolymerization inhibitor) |
15 μM | [55] |
| Cytochalasin D (CytD) | Inhibit macropinocytosis, clathrin- and caveolae-dependent endocytosis (Inhibit F-actin rearrangement) |
1–30 μM | [56–58] |
| N-Ethylmaleimide (NEM) | Inhibit clathrin- and caveolin-dependent endocytosis (Inhibit endosomal fusion, energy metabolism) |
0.1–3 mM | [59–61] |
| Methyl-β-cyclodetritrin (MβCD) | Inhibit clathrin- and caveolae-dependent endocytosis (Deplete or sequester cholesterol) |
2 mM | [62] |
| Filipin | Inhibit caveolae-dependent endocytosis (Inhibit lipid raft; cholesterol binding) |
5 μg/mL | [63] |
| Nystatin | Inhibit caveolae-dependent endocytosis (Inhibit lipid raft; sequester cholesterol) |
5 μg/mL | [63] |
| Wortmannin | Inhibit receptor-mediated endocytosis (Inhibit PI-3 kinase) |
100 nM | [64] |
| 5-(N-Ethyl-N-isopropyl)-amiloride (EIPA) | Inhibit micropinocytosis (Inhibit Na+/H+ exchanger) |
100 μM | [65] |
| Dextran sulfate | Inhibit binding of CPP to cell membrane | 5 μg/mL | [66] |
| DMSO/ethanol | Direct membrane translocation enhancer | 10%/1% | [43] |
| Oleic acid/limonene/PEG | All direct membrane translocation enhancers | 5% | [28, 43] |
| Chloroquine | Lysosomotropic agent (Cause vesicular lysis) |
100 & 25 μM | [67, 68] |
| Ammonium chloride | Inhibit the fusion of lysosomes with endosomes | 10 mM | [67, 69] |