Autophagy
Autophagy is a process by which a cell breaks down macromolecules in response to starvation or stress signals. While it is closely linked with apoptosis, autophagy is primarily characterized as a catabolic mechanism by which cellular energy homeostasis is maintained.
Autophagy Inhibitors |
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Cat. No. | 产品名称/活性 |
4265 | AS 1842856 |
Potent and selective Foxo1 inhibitor; suppresses autophagy | |
6324 | Autophinib |
Potent VPS34 inhibitor | |
3771 | Azithromycin |
Autophagy inhibitor; antibiotic | |
1334 | Bafilomycin A1 |
H+-ATPase (vacuolar) inhibitor; also inhibits autophagy | |
1544 | (±)-Bay K 8644 |
L-type Ca2+ channel activator; inhibits autophagy | |
4109 | Chloroquine diphosphate |
Inhibits apoptosis and autophagy | |
2656 | Concanamycin A |
H+-ATPase (vacuolar) inhibitor | |
4545 | E 64d |
Cathepsin inhibitor; interferes with autolysosomal digestion | |
2473 | GW 4064 |
Selective farnesoid X receptor (FXR) agonist; suppresses autophagy in nutrient-deprived hepatocytes | |
5648 | Hydroxychloroquine sulfate |
Autophagy inhibitor; also TLR9 inhibitor | |
1130 | LY 294002 hydrochloride |
Prototypical PI 3-kinase inhibitor; inhibits autophagic sequestration | |
3982 | Mdivi 1 |
Autophagy inhibitor; also selective dynamin inhibitor | |
3977 | 3-Methyladenine |
Class III PI 3-kinase inhibitor; also inhibits autophagy | |
5153 | ML 240 |
ATP-competitive inhibitor of p97 ATPase; impairs autophagosome maturation | |
5134 | MRT 67307 dihydrochloride |
Autophagy inhibitor; potent ULK inhibitor; also salt inducible kinase (SIK) inhibitor; | |
5067 | MRT 68601 hydrochloride |
Potent TBK1 inhibitor; also inhibits autophagy | |
5780 | MRT 68921 dihydrochloride |
Autophagy inhibitor; potent ULK inhibitor | |
6180 | NMS 873 |
Potent and selective p97 ATPase (VCP) allosteric inhibitor | |
1228 | Nocodazole |
Microtubule inhibitor; inhibits autophagosome-lysosome fusion | |
1190 | Pepstatin A |
Protease inhibitor; interferes with autolysosomal digestion | |
1965 | Simvastatin |
Autophagy inhibitor; HMG-CoA reductase inhibitor; also AMPK activator | |
5197 | Spautin 1 |
Inhibits autophagy; USP10 and USP13 inhibitor | |
1097 | Taxol |
Promotes assembly and inhibits disassembly of microtubules | |
1256 | Vinblastine sulfate |
Disrupts microtubules; inhibits autophagosome maturation | |
1232 | Wortmannin |
Potent, irreversible inhibitor of PI 3-kinase. Also inhibitor of PLK1 | |
4686 | Xanthohumol |
p97 ATPase (VCP) inhibitor; impairs autophagosome maturation | |
Autophagy Activators |
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Cat. No. | 产品名称/活性 |
3336 | A 769662 |
Autophagy activator; potent AMPK activator | |
1234 | A23187, free acid |
Causes ER stress; can be used to induce autophagy in mammalian cells | |
7680 | ABT 263 |
Induces autophagy; Bcl-2 family inhibitor | |
7699 | AUTAC4 |
Autophagy-targeting Degrader; targets dysfuntional mitochondria for degradation; ligand of the translocator protein (TSPO) | |
1231 | Brefeldin A |
Causes ER stress; induces autophagy in mammalian cells | |
4098 | Carbamazepine |
Induces autophagy by inhibiting inositol synthesis; Inhibits neuronal NaV channels | |
0690 | Clonidine hydrochloride |
α2 agonist and I1 ligand; thought to enhance autophagy | |
1126 | Dexamethasone |
Anti-inflammatory glucocorticoid; also induces autophagy in ALL cell lines | |
3093 | Dorsomorphin dihydrochloride |
Induces autophagy via an AMPK inhibition-independent mechanism | |
7474 | EN6 |
Activator of autophagy; inactivates mTORC1 signaling | |
6188 | Everolimus |
Autophagy activator; mTOR inhibitor | |
8072 | FK 866 |
Induces apoptosis and autophagy; potent and non-competitive NAMPT inhibitor | |
0741 | GF 109203X |
Protein kinase C inhibitor | |
0681 | L-690,330 |
Inositol monophosphatase inhibitor; induces autophagy independently of mTOR inhibition | |
6617 | LYN 1604 dihydrochloride |
Induces autophagy; ULK1 agonist | |
2864 | Metformin hydrochloride |
Activator of LKB1/AMPK; activates autophagy | |
1391 | NF 449 |
Highly selective P2X1 antagonist; Gsα-selective antagonist | |
4079 | Niclosamide |
STAT3 inhibitor; also inhibits mTORC1 signaling. Stimulates autophagy in vitro | |
0600 | Nimodipine |
Induces autophagy; Ca2+ channel blocker (L-type) | |
6087 | Perifosine |
PKB/Akt inhibitor; induces autophagy | |
2930 | PI 103 hydrochloride |
Inhibitor of PI 3-kinase, mTOR and DNA-PK | |
1267 | Pifithrin-α hydrobromide |
p53 inhibitor | |
1292 | Rapamycin |
mTOR inhibitor; induces autophagy | |
1418 | Resveratrol |
Autophagy activator; also cyclooxygenase inhibitor | |
0695 | Retinoic acid |
Autophagy activator; also endogenous retinoic acid receptor agonist | |
0790 | Rilmenidine hemifumarate |
α2 agonist and I1 ligand; thought to enhance autophagy | |
1610 | Rottlerin |
Stimulates autophagy | |
4652 | SAHA |
Autophagy activator; also Class I and II HDAC inhibitor | |
4297 | SMER 28 |
Positive regulator of autophagy | |
7558 | SRT 1720 |
Induces autophagy; SIRT1 activator | |
2706 | Temozolomide |
DNA-methylating antitumor agent; also induces autophagy | |
5264 | Temsirolimus |
Autophagy activator; mTOR inhibitor | |
1138 | Thapsigargin |
Causes ER stress; can be used to induce autophagy in mammalian cells | |
4247 | Torin 1 |
Potent and selective mTOR inhibitor; induces autophagy in HeLa cells | |
4248 | Torin 2 |
Autophagy activator; also potent and selective mTOR inhibitor | |
1406 | Trichostatin A |
Autophagy activator; potent histone deacetylase inhibitor | |
3516 | Tunicamycin |
Causes ER stress; can be used to induce autophagy | |
2815 | Valproic acid, sodium salt |
Reduces inositol levels; induces autophagy | |
0654 | Verapamil hydrochloride |
Ca2+ channel blocker (L-type); induces autophagy | |
7878 | XIE62-1004 |
Inducer of autophagy via interaction of p62 and LC3 |
Autophagy is a process by which a cell breaks down macromolecules in response to starvation or stress signals. While it is closely linked with apoptosis, autophagy is primarily characterized as a catabolic mechanism by which cellular energy homeostasis is maintained, and by which cellular organelles and proteins are degraded.
Autophagy also occurs in response to similar stresses to those which induce apoptosis and several proapoptotic signals also induce autophagy - for example, TRAIL, ceramide and the DAPk (death-associated protein kinase) family. However, the way in which the cell is degraded differs: autophagy makes use of the cell's integral lysosomal machinery; apoptosis instead makes use of phagocytic cell lysosomes. These two mechanisms are characteristic of each process and help distinguish them under the microscope.
By enabling the degradation of organelles and macromolecules, autophagy helps provide cells with nutrients under starvation conditions. It assists in the removal of damaged mitochondria and proteins too large to be degraded by the ubiquitin-proteasomal system, as well as helping to maintain whole body homeostasis by removing irreversibly damaged cells. Under conditions such as infection and protein aggregation, this capacity to break down cellular components may also aid cell survival and alleviate neurodegeneration. Compromised autophagy can result in the aggregation of tau, α-synuclein and mutant huntingtin protein fragments, all of which are autophagy substrates and which are linked to neurodegenerative disease. In addition, defective autophagy has been linked to metabolic disorders (such as diabetes and obesity) and aging. Autophagy has also been linked to cancer development - it helps maintain nutrient-deprived cells located in the center of tumors. Autophagy can be used as a target for combination therapies, in particular those which inhibit autophagy and promote apoptosis instead. The roles of autophagy in cancer are complex and often contrasting, and may vary during disease progression. As a result, the targeting of autophagy to treat cancer is more likely to be context-dependent, unlike other tumor processes such as cell growth, angiogenesis and apoptosis.
Intracellular control over autophagy is largely transduced by mTOR and PI 3-K signaling. mTORC1 is directly responsible for autophagy regulation and acts as an autophagy suppressor downstream of the class I PI 3-K-Akt pathway. Nutrient deprivation suppresses kinase activity, thus activating autophagy; AMPK activation inhibits mTOR-dependent signaling, therefore stimulating autophagy. mTOR-independent pathways involved in autophagy also exist, including calpain and inositol, but their mechanisms are yet to be fully elucidated.
Autophagy Webinar
From Fundamental Mechanisms to Mechanical Stress in Physiology and Disease
Mechanical stress is important in the physiological functioning of many organs, and autophagy is known to be one of the major cell stress responses. In this webinar Dr Patrice Codogno discusses current perspectives and novel insights about the molecular events that regulate mammalian autophagosome biogenesis, and the role of autophagy in response to mechanical stress.
Watch Now!Literature for Autophagy
Tocris offers the following scientific literature for Autophagy to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Programmed Cell Death Poster
There are two currently recognized forms of programmed cell death: apoptosis and necroptosis. This poster summarizes the signaling pathways involved in apoptosis, necroptosis and cell survival following death receptor activation, and highlights the influence of the molecular switch, cFLIP, on cell fate.