Autophagy Inducers and Inhibitors

Small molecules able to inhibit or induce autophagic activity provide a mechanism to modulate and study autophagy at the single cell and organismal level. In contrast to genetic models, pharmacological agents allow temporal and dose control. Moreover, often the effects of autophagy modulating agents are reversible. For animal model systems, targeted delivery of small molecules-autophagy modulators to specific organs and tissues may represent a significant advantage.

Small Molecule Modulators	Mode of Action
3-Methyladenine	AMPK inhibitor
(±)-Bay K 8644	L-type Ca2+ channel activator
Spautin 1	USP10 and USP13 inhibitor
LY 294002, Wortmannin	VPS34 inhibitor
MRT 67307, MRT 68921	ULK inhibitor
Simvastatin, A 769662	AMPK activator
Rapamycin*, Torins (1 and 2) Everolimus, PI 103	mTOR inhibitor
Dexamethasone	Anti-inflammatory glucocorticoid; may act via mTOR pathway
L-690,330	Inositol monophosphatase inhibitor; independent of mTOR inhibition
Dorsomorphin	AMPK inhibition-independent
A23187 free acid, Brefeldin A Thapsigargin, Tunicamycin	Causes ER stress
Amiodarone	Causes mitochondrial fragmentation and cell death
GF 109203X	Protein kinase C inhibitor
NF 449*	Highly selective P2X1 antagonist; Gsα-selective antagonist
Perifosine	PKB/AKT inhibitor

*Commonly used modulators. Autophagy modulators available at Tocris: www.tocris.com/autophagy

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