Inducers and Inhibitors

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: http://ift.tt/2qFKGiP

Specific Induction of Autophagy: Autophagy Inducing peptides

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