Table 1 List of the inhibitors used and rationale for their usage, signaling cascade relevance, used concentration (conc.), and 50% inhibitory concentration (IC50)

1

Dynasore

Dynamin inhibitor

10 µM

15 µM

Dynamin-dependent clathrin-mediated endocytosis, but also implicated in phagocytosis, flotillin-, caveolin-dependent ones.

2

MiTMAB

Dynamin inhibitor II

10 µM

3.1 µM

Dynamin-dependent clathrin-mediated endocytosis, but also implicated in phagocytosis, flotillin-, caveolin-dependent ones.

3

Dyngo®4a

Dynamin inhibitor

10 µM

5.5 µM

Dynamin-dependent clathrin-mediated endocytosis, but also implicated in phagocytosis, flotillin-, caveolin-dependent ones.

4

Amiloride

Na⁺/K⁺ exchange inhibitor

2 mM

2–30 µM

Macropinocytosis blocker, inhibiting the Na⁺/K⁺ exchanger, but also antagonizing the formation of submembranous acidification zones⁸².

5

NSC23766

Rac1 GTPase inhibitor

100 μM

50 µM

Rac1 activity is modulated by PLY. Rac1 regulates some forms of membrane clathrin-independent endocytosis⁸³.

6

C3 transferase

RhoA GTPase inhibitor

0.1 μg/ml

1 ng/ml

RhoA activity is modulated by PLY. RhoA can alter transferrin-mediated endocytosis⁸⁴.

7

Ouabain

Na⁺/K⁺-ATPase & submembranous acidification blocker

10 µM

1 µM

Pore formation by PLY may cause cell swelling, leading to secondary activation of the Na⁺/K⁺-ATPase and to the boost of various endocytotic mechanisms⁸⁵.

8

Go6983

PKC inhibitor

1 µM

7–60 nM

Protein kinase C plays a role in some PLY effects and can boost clathrin-dependent endocytosis⁸⁶.

9

GSK690693

Akt/PKCε inhibitor

10 µM

10–20 nM

Activated Akt⁸⁷ and PKCε⁸⁸ play a role in several forms of endocytosis.

10

PP2

Src-kinase inhibitor

10 µM

4–5 nM

PLY activates Src-kinases. The activated Src-kinases Fyn and Syk can stimulate endocytosis and alter cellular volume control⁸⁹.

11

Wortmannin

PI3 kinase inhibitor

10 µM

2–4 nM

Membrane-associated PIP/PIP2/PIP3 signaling. Blocks the phosphorylation of PIP2 to PIP3. The latter participates in small GTPase and Akt membrane recruitment, which can alter secondarily clathrin-independent and dynamin-dependent endocytosis pathways⁶³.

12

U73122

PLC inhibitor

10 µM

1–5 µM

Membrane-associated PIP/PIP2/PIP3 signaling. Blocks membrane-associated PIP2 splitting into IP3 and DAG, which can activate downstream PKC and alter endocytosis⁶³.

13

bpV(pic)

PTEN inhibitor

2 µM

31 nM

Membrane-associated PIP/PIP2/PIP3 signaling. Blocks the transition of PIP3 to PIP2 and shifts the balance of PIP2-PIP3, which affects multiple endocytosis pathways⁶³.

14

Ca²⁺-depletion

Ion

0

Block of Ca-dependent endocytosis by some small pore-forming toxins⁹⁰.

15

K⁺-depletion

Ion

0

Membrane hyperpolarization, clathrin-coated pit reduction⁹¹.