Table 2 Uptake inhibitor overview

From: An anionic, endosome-escaping polymer to potentiate intracellular delivery of cationic peptides, biomacromolecules, and nanoparticles

Inhibitor

Uptake pathway inhibited

Mechanism of action

Dose

Dynasore

Clathrin-mediated endocytosis

Dynamin inhibitor—prevents fission and internalization of clathrin coated vesicles

100 µM

Wortmannin

Macropinocytosis

Phosphatidylinositol-3-kinase (PI3K) inhibitor—PI3K is involved in a variety of actin-dependent processes associated with macropinocytosis

100 nM

5-(N-thyl-N-isopropyl) amiloride (EIPA)

Macropinocytosis

NA+/H+ exchange inhibitor—lowers submembranous pH and prevents Rac1 and Cdc42 signaling

50 µM

Cytochalasin D

Macropinocytosis

Binds to actin, altering and decreasing actin polymerization

50 µM

Methyl-β-cyclodextrin (MβCD)

Lipid raft-mediated endocytosis

Sequesters and depletes cholesterol from cell membranes

5 mM

Dextran sulfate

Scavenger receptor-mediated endocytosis

Competitively binds to scavenger receptors

100 µg/mL

Latrunculin A

Immunological/macrophage phagocytosis

Red sea sponge toxin that binds monomeric actin and prevents actin polymerization

50 µM

  1. The uptake pathways affected by and underlying mechanism of action of the range of uptake inhibitors utilized