Autophagy
Autophagy is a conserved cellular degradation and recycling process in the lysosome. In mammalian cells, there are three primary types of autophagy: microautophagy, macroautophagy, and chaperone-mediated autophagy (CMA). Microphagy captures cargoes by means of invaginations or protrusions of the lysosomal membrane directly, CMA uses chaperones to identify cargo proteins and then unfolds and transfers them into the lysosomal, while macroautophagy sequesters cargo by autophagosomes-de novo synthesized of double-membrane vesicles-and subsequently transport it to the lysosome.
Macroautophagy is the best studied and it occurs at a low level constitutively and can also be further induced under stress conditions, such as nutrient or energy starvation with a salient feature of autophagy protein degradation. Stress-induced macrophagy plays an important role in protein catabolism with another key protein degradation pathway, the ubiquitin–proteasome system (UPS).
As the study progressed, autophagy gains its importance under basal, nutrient-rich conditions, and is now recognized as a critical housekeeping pathway in catabolism of diverse cellular constituents, such as protein aggregates (aggrephagy), lipid droplets (lipophagy), iron complex (Ferritinophagy) and carbohydrate. Except for macromolecules, autophagy can also target several organelles and structures, such as mitochondria (mitophagy), peroxisome (pexophagy), endoplasmic reticulum (reticulophagy or ER-phagy), ribosome (ribophagy), spermatozoon-inherited organelles following fertilization (allophagy), secretory granules within pancreatic cells (zymophagy) and intracellular pathogens (xenophagy).
Autophagy and its dysfunction are associated with a variety of human pathologies, including ageing, cancer, neurodegenerative disease, heart disease and metabolic diseases, such as diabetes. Plenty of drugs and natural products are involved in autophagy modulation through multiple signaling pathways. Small molecules that can regulate autophagy seem to have great potential to intervene such diseases in animal models or clinical courses.
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Autophagy Inhibitors
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Autophagy Ligand
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Autophagy Related Products (3425)
Related Products (3425)
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Antibodies (31)
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Autophagy Signaling Pathway
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Imipramine-d4
0 ImagesCat. No.: HY-B1490AS1CAS No.: 96705-18-9Imipramine-d4 is deuterium labeled Imipramine. Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.
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Harmol hydrochloride
0 ImagesCat. No.: HY-107811ACAS No.: 40580-83-4Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol hydrochloride can induce cell mitosis, Autophagy and Apoptosis. Harmol hydrochloride promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol hydrochloride has anti-tumor, anti-depressant and anti-aging activities. Harmol hydrochloride improves motor impairment in a mouse Parkinson's disease model.
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Curdione (Standard)
0 ImagesCat. No.: HY-N0353RCAS No.: 13657-68-6Synonyms: (+)-Curdione (Standard)Curdione (Standard) is the analytical standard of Curdione. This product is intended for research and analytical applications. Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
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Bortezomib (GMP)
0 ImagesCat. No.: HY-10227GSynonyms: PS-341 (GMP); LDP-341 (GMP); NSC 681239 (GMP)Bortezomib (GMP) (PS-341 (GMP)) is Bortezomib (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM). Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs).
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Dasatinib (GMP Like)
0 ImagesCat. No.: HY-10181GLCAS No.: 302962-49-8Synonyms: BMS-354825 (GMP Like)Dasatinib (GMP Like) (BMS-354825 (GMP Like)) is Dasatinib (HY-10181) produced by using GMP like guidelines. GMP Like small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
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Fenofibrate-d4
0 ImagesCat. No.: HY-17356S1CAS No.: 1092484-57-5Fenofibrate-d4 is the deuterium labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
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SH498
0 ImagesCat. No.: HY-143658CAS No.: 2125724-38-9SH498, a novel Bmi-1-mediated antitumor agent, shows potent antiproliferative activity.
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RK-682 hemicalcium
0 ImagesCat. No.: HY-135564CAS No.: 332131-32-5RK-682 hemicalcium is the hemicalcium salt form of RK-682 (HY-135564A). RK-682 hemicalcium is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 hemicalcium inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 hemicalcium inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24[2].
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(Rac)-Lonafarnib
0 ImagesCat. No.: HY-15136BCAS No.: 193275-86-4Synonyms: Sch66336 racemate(Rac)-Lonafarnib (Sch66336 racemate) is an isomer of Lonafarnib (HY-15136). Lonafarnib (Sch66336) is an orally active, blood-brain barrier penetrant farnesyltransferase (FPTase) inhibitor. Lonafarnib increases the phosphorylation levels of Akt, CaMKII and CREB, upregulates BDNF expression in the hippocampus, elevates the content of α7nAChR on cell membranes, and blocks the isoprenylation of H-Ras. Lonafarnib repairs synapses and reverses spatial memory deficits in Aβ1-42 model mice. Lonafarnib inhibits RSV fusion and replication, and alleviates virus-induced lung injury. Lonafarnib activates the lysosomal and autophagic pathways, and reduces the phosphorylation and aggregation of tau. Lonafarnib acts synergistically with Sorafenib (HY-10201) to promote apoptosis, and inhibits the proliferation and invasion of melanoma cells. Lonafarnib inhibits the farnesylation of progerin, repairs nuclear membrane defects, and activates the cGAS-STING-STAT1 signaling pathway. Lonafarnib can be used in research related to diseases including Alzheimer's disease, viral infections, melanoma, and progeria.
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Pepstatin (Standard)
0 ImagesCat. No.: HY-P0018RCAS No.: 26305-03-3Synonyms: Pepstatin A (Standard)Pepstatin (Standard) is the analytical standard of Pepstatin. This product is intended for research and analytical applications. Pepstatin (Pepstatin A) is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin also inhibits HIV protease[1][2].
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Anticancer agent 296
0 ImagesCat. No.: HY-181087Anticancer agent 296 is a potent anticancer agent that activates the PERK-eIF2α-CHOP signaling pathway to induce endoplasmic reticulum stress, thereby regulating caspase and Bcl-2 family proteins, ultimately leading to apoptosis. Anticancer agent 296 increases intracellular levels of reactive oxygen species (ROS), reduces mitochondrial membrane potential, and promotes Ca2+ release. Anticancer agent 296 suppresses cell colony formation and S-phase cell proliferation, and induces autophagy. Anticancer agent 296 is applicable for research on non-small cell lung cancer (NSCLC).
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Thalidomide-NH-(CH2)3-NH-Boc
0 ImagesCat. No.: HY-W584515CAS No.: 2093386-36-6Thalidomide-NH-(CH2)3-NH-Boc is a Boc-modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)3-NH-Boc is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules targeting 11β-substituted estradiol.
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DS-PPE-GW
0 ImagesCat. No.: HY-180218DS-PPE-GW is a BCR-ABL ATTEC degrader. DS-PPE-GW connects BCR-ABL and LC3B, thereby tethering BCR-ABL to the autophagosome membrane. DS-PPE-GW shows potent BCR-ABL degradation. DS-PPE-GW has anticancer activity against chronic myeloid leukemia (Pink: LC3B ligand (HY-10542); Blue: BCR-ABL ligand (HY-107447); Black: Linker (HY-W001860)).
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DCAP (Standard)
0 ImagesSynonyms: VU0607402 (Standard)Diphenylcyclopropenone (Standard) is the analytical standard of Diphenylcyclopropenone. This product is intended for research and analytical applications. Diphenylcyclopropenone (Diphencyprone) is a topical immunomodulatory agent that can be used for alopecia areata research.
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Thalidomide-O-C3-NH2
0 ImagesCat. No.: HY-138847CAS No.: 2509360-22-7Thalidomide-O-C3-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
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MAAAHR
0 ImagesCat. No.: HY-P12279MAAAHR is a neuroprotective agent. MAAAHR is isolated and purified from C-phycocyanin of Spirulina platensis. MAAAHR induces antioxidant gene expression through activating the Nrf2 signaling pathway. MAAAHR inhibits excessive Autophagy by reducing the expression of proteins such as α-Syn and Parkin. MAAAHR inhibits Apoptosis. MAAAHR scavenges excessive ROS, enhances SOD, CAT, and GSH-Px activities, and reduces protein carbonyl content. MAAAHR inhibits Acetylcholinesterase. MAAAHR protects zebrafish against MPTP (HY-15608)-induced dopaminergic neuronal and neurovascular loss and alleviates motor impairment. MAAAHR can be used for research on Parkinson's disease.
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Aspirin-d7
0 ImagesCat. No.: HY-W707656Aspirin-d7 is the deuterium labeled Aspirin (HY-14654). Aspirin (Acetylsalicylic acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
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HDAC-IN-36
0 ImagesCat. No.: HY-146684CAS No.: 2482992-54-9
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Ambrosin
0 ImagesAmbrosin is an orally active NF-κβ and BACE1 inhibitor. Ambrosin reduces pro-inflammatory and nitrosative mediators, increases PPARγ levels, inhibits apoptosis (Apoptosis), enhances autophagy (Autophagy), and ameliorates oxidative stress. Ambrosin reduces Amyloid plaque deposition. Ambrosin improves lipopolysaccharide-induced memory impairment and colonic histopathological changes. Ambrosin can be used in research related to Alzheimer's disease and colitis.
