Common chemical and pharmaceutical endocytosis inhibitors.

Endocytosis inhibitors	Pathway(s) involved	Mechanism	Limitation	Conc. rangea	Ref.
Hypertonic sucrose	CME	Traps clathrin in microcages	Interferes with macropinocytosis	0.4–0.5 M	167
Potassium depletion		Removes clathrin lattices that associate with cell membrane	Affects actin cytoskeleton	n/a	167 and 173
Cytosol acidification		Inhibits the scission of CCPs from the cell membrane	Affects actin cytoskeleton and interferes with macropinocytosis	10–30 mM NH4Cl	174 and 175
CPZ		AP2 inhibitor; blocks endosome recycling	Affects biogenesis of large intracellular vesicles such as phagosomes and macropinosomes	50–100 μM	176
MDC		Stabilizes CCVs	Global changes in the dynamics of the actin cytoskeleton	100–300 μM	177 and 178
Phenylarsine oxide		Inhibits protein tyrosine phosphatases; exact mechanism remains unknown	Inhibits phagocytosis and macropinocytosis	1–20 μM	178
Chloroquine		Reduces the expression of phosphatidylinositol binding clathrin assembly protein (PICALM)	May only affect phagocytic cells and interfere with other endocytic mechanisms	20–400 μM	179
Monensin		Dissipation of a proton gradient	Interferes with endocytic trafficking such as receptor recycling	5–40 μM	180 and 181
ES9-17		Inhibitor of the CHC function; cytosol acidification	Still unknown (discovered recently)	30 μM	182
Pitstop 2		Interferes with binding of proteins to the N-terminal domain of clathrin	Affects most endocytic pathways	10–100 μM	170 and 174
Methyl-β-cyclodextrin	Caveolae-mediated endocytosis/lipid rafts	Cholesterol depletion from the cell membrane	Interferes with macropinocytosis and CME	5–10 mM	183
Filipin		Interacts with cholesterol at the cell membrane	Inhibits CME; unstable and toxic at high concentrations	1–5 μg mL−1	184
Statins		Blocks cholesterol synthesis	Affects most endocytic mechanisms	10–100 μM	185
Genistein		Inhibits several tyrosine kinases	Interferes with dynamin and may affect other endocytic processes	200–400 μM	81, 172 and 186
CytD and lantruculins	Phagocytosis and macropinocytosis	Block actin polymerization	Affect most endocytic mechanisms	1–10 μM	60 and 187
Amiloride or its derivatives (EIPA and HOE-694)		Na+/H+ exchanger pump inhibitor; blocks Rac1 and Cdc42 signaling	Inhibit CME	1 mM for amiloride and 50–100 μM for its derivatives	188 and 189
Imipramine		Inhibits plasma membrane ruffle formation	Still unknown (the mechanism of inhibition is still not fully understood)	5 μM	190 and 191
Wortmannin and LY294002		Inhibit the activity of phosphatidylinositol 3-kinase	Affect most endocytic mechanisms	10 nM–10 μM for Wortmannin and 20 μg mL−1 for LY294002	164, 192 and 193
Rottlerin		Inhibits the activity of protein kinase C delta	Affects most endocytic mechanisms	1–3 μM	194 and 195
Dynasore, dynole and dyngo compounds	Dynamin-dependent endocytosis	Inhibit the GTPase activity of dynamin1 and 2	May interfere with cholesterol homeostasis and actin	1–500 μM	196 and 197

^aThe concentration of inhibitor is cell- and time-dependent.