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. 2019 Nov 11;11(11):1775. doi: 10.3390/cancers11111775

Table 1.

Examples of pharmacological autophagy inhibitors.

Name Mechanism of Action Targeted Stage in Autophagy Ref.
Inhibitors that target late stages of autophagy
Lys05 Lysosomotropic agent

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [46,47]
Chloroquine (CQ) Lysosomotropic agent

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [48,49]
Hydroxychloroquine (HCQ)
Quinacrine (QNX)
IITZ-01 Lysosomotropic agent

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [50]
ROC-325 unknown

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [51,52,53]
Bafilomycin A1 (Baf A1) Vacuolar ATPase inhibitor

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [54]
ECDD-S27 Vacuolar ATPase inhibitor

  • Lysosomal acidification

  • Autophagosome-lysosome fusion

 [55]
Ca-5f Unknown

  • Autophagosome-lysosome fusion

 [56]
EACC Syntaxin 17 (STX17) translocation inhibitor

  • Autophagosome-lysosome fusion

 [57]
MHY1485 Mammalian target of rapamycin (mTOR) activator

  • Autophagosome-lysosome fusion

 [58]
Pepstatin A Acid protease inhibitor

  • Lysosomal proteolysis

 [59,60]
E64-d Acid protease inhibitor

  • Lysosomal proteolysis

 [59,60]
Alpha-hederin Unknown

  • Lysosomal proteolysis

 [61]
Inhibitors that target early stages of autophagy
SB02024 Vacuolar protein sorting protein 34 (Vps34) inhibitor

  • Autophagosome formation

 [62]
SAR405 Vacuolar protein sorting protein 18 and 34 (Vps18 and Vps34) inhibitor

  • Autophagosome formation

 [63]
PIK-III Vacuolar protein sorting protein 34 (Vps34) inhibitor

  • Autophagosome formation

 [64]
Autophinib Vacuolar protein sorting protein 34 (Vps34) inhibitor

  • Autophagosome formation

 [65]
SBI-0206965 Unc-51-like kinase 1 (ULK1) inhibitor

  • Autophagosome formation

 [66]
ULK-100, ULK-101 Unc-51-like kinase 1 (ULK1) inhibitor

  • Autophagosome formation

 [67]
LY294002 Phosphoinositide 3-kinase (PI3) inhibitor

  • Autophagosome formation

 [68,69]
3-Methyladenine (3-MA) Phosphoinositide 3-kinase (PI3) inhibitor

  • Autophagosome formation

 [70]
Wortmannin Phosphoinositide 3-kinase (PI3) inhibitor

  • Autophagosome formation

 [68,71,72]
Spautin-1 Ubiquitin Specific Peptidase 10 and 13 (USP10 and USP13) inhibitor

  • Autophagosome formation

 [73,74]
NSC185058 Autophagy-related (ATG) protein 4A and 4B (ATG4A and ATG4B) inhibitor

  • LC3B, GABARAPL2 priming

  • Autophagosome formation

 [75]
UAMC-2526 Autophagy-related (ATG) protein 4B (ATG4B) inhibitor

  • LC3B priming

  • Autophagosome formation

 [76]
DMP-1 unknown

  • LC3B lipidation

  • Autophagosome formation

 [77]
Inhibitors that target both early and late stages of autophagy
Tioconazole Autophagy-related (ATG) protein 4A and 4B (ATG4A and ATG4B) inhibitor

  • LC3B, GABARAPL2 priming

  • LC3B delipidation

  • Autophagosome-lysosome fusion

 [78]
LV-320 Autophagy-related (ATG) protein 4A and 4B (ATG4A and ATG4B) inhibitor

  • LC3B priming

  • LC3B delipidation

  • Autophagosome-lysosome fusion

 [79]
S130 Autophagy-related (ATG) protein 4A and 4B (ATG4A and ATG4B) inhibitor

  • LC3B, GABARAPL2 priming

  • LC3B delipidation

 [80]
Xanthium strumarium Fruit Extract Autophagy-related (ATG) protein 4B (ATG4B) inhibitor

  • LC3B, GABARAPL2 priming

  • LC3B delipidation

 [81]
Verteporfin unknown

  • Autophagosome formation

  • Autolysosome degradation

 [82]