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Autophagy

Autophagy is the natural, regulated mechanism of the cell that removes unnecessary or disfunctional components. It allows the orderly degradation and recycling of cellular components. Three forms of autophagy are commonly described: macroautophagy, microautophagy, and chaperone-mediated autophagy (CMA). In macroautophagy, expendable cytoplasmic constituents are targeted and isolated from the rest of the cell within a double-membraned vesicle known as an autophagosome, which, in time, fuses with an available lysosome, bringing its specialty process of waste management and disposal; and eventually the contents of the vesicle (now called an autolysosome) are degraded and recycled.

  • Chloroquine
    T868954-05-7
    Chloroquine is a Toll-like receptor inhibitor that inhibits autophagy. Chloroquine has anti-malarial and anti-inflammatory activity and is widely used in the treatment of malaria and rheumatoid arthritis. Chloroquine also has anti-SARS-CoV-2 (COVID-19) activity and anti-HIV-1 activity.
    • $43.2
    • $54
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  • PX-478
    T6961685898-44-6
    PX-478 is a HIF-1α inhibitor with selectivity, oral activity, and blood-brain barrier permeability. PX-478 has antitumor activity and also protects pancreatic β-cell function in diabetes mellitus and is used in type 2 diabetes mellitus research.
    • $48
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  • Regorafenib
    T1792755037-03-7
    Regorafenib (BAY 73-4506) is a multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ and is orally active. Regorafenib has antitumor and anti-angiogenic activity.
    • $30
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • Curcumin
    T1516458-37-7
    Curcumin (Natural Yellow 3) is a phenolic natural product, an inhibitor of histone acetyltransferase p300/CREB (IC50=25 μM) with specificity. Curcumin has a wide range of pharmacological activities such as antitumor, anti-inflammatory and antioxidant.
    • $30
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • Sorafenib
    T0093L284461-73-0
    Sorafenib (Bay 43-9006) is a multikinase inhibitor that inhibits Raf-1, B-Raf, VEGFR2, VEGFR3, VEGFR4, PDGFRβ, FLT3, c-Kit, and others (IC50=6/22/90/15/20/20/57/58 nM) with oral activity. Sorafenib has antitumor activity and can induce autophagy and apoptosis as well as agonistic ferroptosis.
    • $34
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    TargetMol | Citations Cited
  • Verteporfin
    T3112129497-78-5
    Verteporfin (BPD-MA) is a YAP inhibitor that inhibits YAP-TEAD interactions. Verteporfin is also a photosensitizer used in photodynamic therapy. Verteporfin also induces apoptosis and inhibits autophagy.
    • $34
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    TargetMol | Inhibitor Hot
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  • Rapamycin
    T153753123-88-9
    Rapamycin (AY 22989) is a natural product of macrolides, an mTOR inhibitor with specificity (HEK293 cells: IC50=0.1 nM). Rapamycin has immunosuppressive activity and induces autophagy.
    • $30
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  • MPP+ iodide
    T916936913-39-0
    MPP+ iodide, the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA)
    • $33
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    TargetMol | Inhibitor Hot
  • ML-SA5
    T600362418670-70-7
    ML-SA5 is an MCOLN1 agonist and arrests autophagic flux by perturbing fusion between autophagosomes and lysosomes.
    • $33
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    TargetMol | Inhibitor Hot
  • Tamoxifen
    T690610540-29-1
    • $39
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    TargetMol | Inhibitor Hot
  • Luminespib
    T1989747412-49-3
    Luminespib (VER-52296) is a new-type inhibitor of HSP90 (IC50s: 7.8 21 nM for HSP90α β in cell free assay).
    • $52
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    TargetMol | Inhibitor Hot
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  • BI-D1870
    T6171501437-28-1
    BI-D1870 is a cell-permeable, ATP-competitive inhibitor of ribosomal S6 kinases (RSKs; IC50s: 31 24 18 15 nM for RSK1 2 3 4).
    • $48
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    TargetMol | Inhibitor Hot
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  • Mdivi-1
    T1907338967-87-6
    Mdivi-1 (Mitochondrial division inhibitor 1) is a mitochondrial division inhibitor that inhibits DRP1 and Dynamin I (IC50=1-10 μM). Mdivi-1 inhibits mitochondrial autophagy.
    • $39
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    TargetMol | Inhibitor Hot
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  • MK-2206 dihydrochloride
    T19521032350-13-2
    MK-2206 dihydrochloride (MK-2206 2HCl) is a variant Akt inhibitor that inhibits Akt1, Akt2, and Akt3 (IC50=8/12/65 nM) with orally active, highly potent and selective potency. MK-2206 dihydrochloride exhibits antitumor activity.
    • $30
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    TargetMol | Inhibitor Hot
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  • Enzalutamide
    T6002915087-33-1
    Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist (IC50=36 nM in LNCaP). Enzalutamide activates autophagy, has antitumor activity, and is commonly used in the treatment of desmoplasia-resistant prostate cancer.
    • $40
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    TargetMol | Inhibitor Hot
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  • (+)-JQ-1
    T21101268524-70-4
    (+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1/2) (IC50=77/33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
    • $30
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    TargetMol | Inhibitor Hot
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  • Bortezomib
    T2399179324-69-7
    Bortezomib (LDP 341) is a 20S proteasome inhibitor (Ki=0.6 nM) that is reversible and selective. Bortezomib has antitumor activity and inhibits NF-κB, which can disrupt the cell cycle and induce apoptosis.
    • $48
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    TargetMol | Inhibitor Hot
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  • CHIR-99021
    T2310252917-06-9
    CHIR-99021 (CT99021) is an activator of the Wnt/β-catenin signaling pathway and a GSK-3α/β inhibitor (IC50=10/6.7 nM) with selective and oral activity.CHIR-99021 induces cellular autophagy, which enhances self-renewal in mouse and human embryonic stem cells.
    • $36
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  • Venetoclax
    T21191257044-40-8
    Venetoclax (ABT-199) is a Bcl-2 inhibitor (Ki<0.01 nM) with potent, selective, and orally active properties. Venetoclax has a 3-order-of-magnitude lower affinity for Bcl-xL and Bcl-W (Kis=48/245 nM). Venetoclax induces autophagy and apoptosis.
    • $48
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  • Elexacaftor
    T149352216712-66-0
    Elexacaftor (VX-445) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR) and it also facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
    • $89
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  • Dexamethasone
    T107650-02-2
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist and an IL receptor modulator. Dexamethasone has anti-inflammatory and immunosuppressive activity and induces autophagy. Dexamethasone inhibits LPS-induced inflammatory responses in macrophages.
    • $45
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  • 3-Methyladenine
    T18795142-23-4
    3-Methyladenine (3-MA) is a PI3K inhibitor that selectively inhibits class IB PI3Kγ (IC50=60 μM) and class III VPS34 (IC50=25 μM). 3-Methyladenine inhibits autophagy.
    • $35
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  • Ruxolitinib
    T1829941678-49-5
    Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
    • $53
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  • Forskolin
    T293966575-29-9
    Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.
    • $36
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  • Doxorubicin hydrochloride
    T102025316-40-9
    Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy.
    • $34
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  • Deferoxamine Mesylate
    T1637138-14-7
    Deferoxamine Mesylate (DFOM) is an iron chelator and ferroptosis inhibitor. Deferoxamine Mesylate binds free iron into a stable complex and reduces iron accumulation. Deferoxamine Mesylate up-regulates HIF-1α levels and induces apoptosis.
    • $31
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  • Temozolomide
    T117885622-93-1
    Temozolomide (TMZ) is a DNA alkylating agent with blood-brain barrier permeability and oral activity. Temozolomide has antitumor activity and antiangiogenic activity, and also induces apoptosis and autophagy. Temozolomide is stable under acidic conditions and hydrolyzes under neutral or slightly alkaline conditions.
    • $42
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  • Bafilomycin A1
    T674088899-55-2
    Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.
    • $287
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  • Oxaliplatin
    T016461825-94-3
    Oxaliplatin (L-OHP) is a DNA alkylating agent, an inhibitor of DNA synthesis. Oxaliplatin causes DNA cross-linking damage, preventing DNA replication and transcription and leading to cell death. Oxaliplatin induces autophagy.
    • $50
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  • MG-132
    T2154133407-82-6
    MG-132 (Z-Leu-Leu-Leu-al) is a 26S proteasome inhibitor (IC50=100 nM) that is cell-permeable and reversible. MG-132 acts as an autophagy activator and also induces apoptosis.
    • $40
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  • Telaglenastat
    T67971439399-58-2
    Telaglenastat (CB 839) (IC50 of 24 nM), an effective, specific, and oral inhibitor, which is bioavailable glutaminase, for recombinant human GAC.
    • $32
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    TargetMol | Inhibitor Hot
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  • Urolithin A
    T71741143-70-0
    Urolithin A is a secondary metabolite of ellagic acid, a polyphenolic antioxidant, that has antiproliferative, anti-inflammatory, and anti-oxidant properties.
    • $42
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    TargetMol | Inhibitor Hot
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  • LY294002
    T2008154447-36-6
    LY294002 (SF 1101) is a broad-spectrum inhibitor of PI3K, inhibiting PI3Kα, PI3Kδ, and PI3Kβ (IC50=0.5/0.57/0.97 μM). LY294002 is also an inhibitor of DNA-PK (IC50=1.4 μM) and an inhibitor of CK2 (IC50=98 nM). LY294002 activates apoptosis and autophagy.
    • $34
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    TargetMol | Inhibitor Hot
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  • Gemcitabine
    T025195058-81-4
    Gemcitabine (LY188011) is a synthetic cytosine nucleoside derivative and an inhibitor of DNA synthesis. Gemcitabine has antitumor and antimetabolic activities. Gemcitabine induces autophagy and apoptosis.
    • $34
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • (E)-Daporinad
    T2644658084-64-1
    (E)-Daporinad (FK866) is a small molecule inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase), with potential antineoplastic and antiangiogenic activities.
    • $36
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    TargetMol | Inhibitor Hot
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  • Vinorelbine ditartrate
    T6213125317-39-7
    Vinorelbine ditartrate (KW-2307), a semi-synthetic vinca alkaloid, interacts with tubulin resulting in mitosis inhibition.
    • $30
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    TargetMol | Inhibitor Hot
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  • Quizartinib
    T2066950769-58-1
    Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
    • $53
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    TargetMol | Inhibitor Hot
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  • Olaparib
    T3015763113-22-0
    Olaparib (KU0059436) is a small molecule inhibitor of PARP1/PARP2 (IC50=5/1 nM), with weak inhibitory activity against PARP tankyrase-1 (IC50=1.5 μM), and is selective and orally active. Olaparib exhibits autophagy and mitochondrial autophagy activation activity.
    • $31
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  • Streptozocin
    T150718883-66-4
    Streptozocin (NSC-85998) is an antibiotic that induces DNA methylation. Streptozocin is toxic to insulin-producing pancreatic islet B-cells and is commonly used in the construction of animal models of type 1 diabetes. The product is unstable in solution and is recommended to be dispensed now.
    • $30
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    TargetMol | Inhibitor Hot
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  • Ruxolitinib phosphate
    T30431092939-17-7
    Ruxolitinib phosphate (INCB018424)(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
    • $44
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    TargetMol | Inhibitor Hot
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  • Obeticholic Acid
    T1789459789-99-2
    Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
    • $41
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    TargetMol | Inhibitor Hot
  • Capivasertib
    T19201143532-39-1
    Capivasertib (AZD5363) is a broad-spectrum AKT inhibitor with inhibitory activity against Akt1, Akt2, and Akt3 (IC50=3/7/7 nM) with oral activity. Capivasertib has antitumor activity for the treatment of breast cancer.
    • $34
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    TargetMol | Inhibitor Hot
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  • GCN2iB
    T113752183470-12-2
    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
    • $77
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    TargetMol | Inhibitor Hot
  • DAPT
    T6202208255-80-5
    DAPT (LY-374973) is a γ-secretase inhibitor that inhibits total Aβ and Aβ42 (IC50=115/200 nM) and is orally active. DAPT is also a Notch inhibitor. DAPT induces cell differentiation, autophagy and apoptosis.
    • $53
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    TargetMol | Inhibitor Hot
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  • Necrostatin-1
    T18474311-88-0
    Necrostatin-1 (Nec-1) is a necrotic apoptosis inhibitor and RIP1 inhibitor with specificity. Necrostatin-1 inhibits TNF-α-induced necrotic apoptosis. Necrostatin-1 also inhibits IDO.
    • $30
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    TargetMol | Inhibitor Hot
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  • Butein
    T6427487-52-5
    Butein (2’,3,4,4’-tetrahydroxy Chalcone), a plant polyphenol, is isolated from Rhus verniciflua. It can inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, and also can inhibit EGFR.
    • $36
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • Atezolizumab
    T99021380723-44-3
    Atezolizumab (anti-PD-L1) is a fully humanized IgG1 monoclonal antibody that blocks the interaction of PD-L1 with both PD-1 and B7.1 but not the interaction of PD-L2 with PD-1.
    • $229
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    TargetMol | Inhibitor Hot
  • Paclitaxel
    T096833069-62-4
    Paclitaxel (Taxol) is a natural product and a microtubule polymer stabilizer. Paclitaxel has anti-tumor activity and causes cell death by inducing mitotic arrest, apoptosis, and cell autophagy.
    • $34
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    TargetMol | Inhibitor Hot
    TargetMol | Citations Cited
  • Cisplatin
    T156415663-27-1
    Cisplatin (CDDP) is a DNA cross-linking agent. Cisplatin has antitumor activity and inhibits DNA synthesis by forming DNA adducts in cancer cells. Cisplatin also activates ferroptosis and induces autophagy.
    • $28
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    TargetMol | Inhibitor Hot
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  • Aloe emodin
    T2843481-72-1
    Aloe emodin (Rhabarberone) is an interferon-inducing agent, for JEV (IC50=1 μg/mL) and EV71(IC50=0.33 μg/mL ).
    • $34
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