2. Signaling Pathways
  3. Autophagy
  4. Autophagy

Autophagy

Autophagy

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-141882
    DC-LC3in-D5
    		Inhibitor 98.62%
    DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy.
    DC-LC3in-D5
  • HY-103706
    ROC-325
    		Inhibitor 98.73%
    ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
    ROC-325
  • HY-N1990
    Gypenoside XLIX
    		Inhibitor 99.88%
    Gypenoside XLIX is a multifunctional bioactive compound that can be isolated from Gynostemma pentaphyllum, with a Ka value of 1.58 μM for its binding to SIRT1. Gypenoside XLIX acts as a PPAR-α agonist. It inhibits the activation of TLR4-mediated NF-κB signaling pathway by activating the Sirt1/Nrf2 signaling pathway, reduces ROS accumulation, and alleviates hepatic inflammatory injury in mice with sepsis-induced liver disease. Gypenoside XLIX targets SIRT1 to block YAP-NLRP3 activation and improve sepsis-induced cardiomyopathy. Gypenoside XLIX inhibits apoptosis (Apoptosis), pyroptosis (Pyroptosis), autophagy (Autophagy), lipid peroxidation, pro-inflammatory cytokines and anti-inflammatory cytokines. Gypenoside XLIX alleviates sepsis-induced splenic injury by inhibiting inflammation and oxidative stress, and mitigates sepsis-associated encephalopathy by targeting PPAR-α. Gypenoside XLIX prevents acute kidney injury by inhibiting IGFBP7/IGF1R-mediated programmed cell death and inflammation. Gypenoside XLIX inhibits the expression and activity of vascular cell adhesion molecule-1 in cytokine-induced human endothelial cells. Gypenoside XLIX is applicable to research related to acute liver injury, lung injury, cardiomyopathy, acute splenic injury, sepsis-associated encephalopathy, acute kidney injury, atherosclerosis and chronic inflammation.
    Gypenoside XLIX
  • HY-B1417
    Nortriptyline hydrochloride
    		Inhibitor 99.98%
    Nortriptyline (Desmethylamitriptyline) hydrochloride, the main active metabolite of Amitriptyline, is a tricyclic antidepressant. Nortriptyline hydrochloride is a potent autophagy inhibitor and has anticancer effects.
    Nortriptyline hydrochloride
  • HY-112698
    CA-5f
    		Inhibitor 99.14%
    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion. CA-5f increases LC3B-II (a marker to monitor autophagy) and SQSTM1 protein, and also increases ROS production. Anti-tumor activity.
    CA-5f
  • HY-136351
    THZ-P1-2
    		Inhibitor 99.86%
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
    THZ-P1-2
  • HY-B0642
    Isosorbide mononitrate
    		Inhibitor 99.95%
    Isosorbide mononitrate (Isosorbide-5-mononitrate) is an orally active nitric acid compound used for angina pectoris by dilating blood vessels and lowering blood pressure. Isosorbide mononitrate increases the viability and proliferation of HUVECs by decreasing Apoptosis and elevated the expressions of vedf, kdrl, pdgfr in zebrafish embryos. Isosorbide mononitrate is promising for research of heart failure and coronary heart disease.
    Isosorbide mononitrate
  • HY-10962
    Momelotinib sulfate
    		Inhibitor 98.63%
    Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
    Momelotinib sulfate
  • HY-N12060
    Ginkgo biloba extract
    		Inhibitor
    Ginkgo biloba extract is a natural product that can be isolated from Ginkgo biloba leaves. Ginkgo biloba extract alleviates oxidative stress-induced neuronal apoptosis (Apoptosis) by stabilizing mitochondrial function, regulating Bcl-2 family proteins and inhibiting caspase activation. Ginkgo biloba extract alleviates testicular injury by upregulating SKP2 and inhibiting Beclin1-independent autophagy (Autophagy). Ginkgo biloba extract alleviates various types of neuronal damage in animal models. Ginkgo biloba extract reduces behavioral sensitization in rats. Ginkgo biloba extract counteracts Aβ-induced neurotoxicity by blocking a series of Aβ-triggered events, including glucose uptake, ROS accumulation, AKT activation, mitochondrial dysfunction, JNK and ERK 1/2 pathways, and apoptosis, and also interferes with the formation of Aβ oligomers. Ginkgo biloba extract is applicable to research related to cerebral hypoperfusion, testicular injury, Alzheimer's disease, Parkinson's disease, multi-infarct dementia, stroke, traumatic brain injury and amyotrophic lateral sclerosis.
    Ginkgo biloba extract
  • HY-N1487
    Oleanonic acid
    		Inhibitor 99.91%
    Oleanonic acid (3-Oxooleanolic acid) is an orally available triterpene that has anti-inflammatory and insecticidal properties. In vitro, oleanonic acid can improve oxidative stress, autophagy defects, ferroptosis, mitochondrial damage, and endoplasmic reticulum stress induced by Amyloid-β, and in vivo, it can alleviate myocardial hypertrophy in rats.
    Oleanonic acid
  • HY-137742
    SBP-7455
    		Inhibitor 98.01%
    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research.
    SBP-7455
  • HY-B0260R
    Methylprednisolone (Standard)
    		Inhibitor
    Methylprednisolone (Standard) is the analytical standard of Methylprednisolone. This product is intended for research and analytical applications. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone (Standard)
  • HY-145371
    ATG7-IN-1
    		Inhibitor 99.84%
    ATG7-IN-1 (Compound 37) is a potent and selective inhibitor of ATG7 (IC50 = 62 nM).
    ATG7-IN-1
  • HY-P0018B
    Pepstatin Ammonium
    		Inhibitor 99.76%
    Pepstatin (Pepstatin A) Ammonium 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 Ammonium also inhibits HIV protease.
    Pepstatin Ammonium
  • HY-B2098
    Lucanthone
    		Inhibitor 99.63%
    Lucanthone is an endonuclease inhibitor of Apurinic endonuclease-1 (APE-1).
    Lucanthone
  • HY-13423
    Tenovin-1
    		Inhibitor 99.88%
    Tenovin-1, a p53 activator, protects p53 from MDM2-mediated degradation. Tenovin-1 acts through inhibition of the protein-deacetylating activities of SirT1 and SirT2. Tenovin-1 is also a dihydroorotate dehydrogenase (DHODH) inhibitor.
    Tenovin-1
  • HY-N10546
    Ganglioside GM1
    		Inhibitor 99.0%
    Ganglioside GM1 is a type of glycosphingolipid, mainly found on the cell membranes of the central nervous system of vertebrates. Ganglioside GM1 exerts neuroprotective effects by reducing excessive activation of NMDAR, activating TrkA and ERK1/2, and inhibiting oxidative stress and cell apoptosis and autophagy. Ganglioside GM1 can be used in the research of diseases such as traumatic brain injury, Parkinson's disease, Alzheimer's disease, and Huntington's disease.
    Ganglioside GM1
  • HY-155994
    PIK5-12d
    		Inhibitor 99.15%
    PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer. (Pink: PIKfyve ligand (HY-175631), Blue: VHL Ligand (HY-125845), Black: Linker, PIKfyve ligand-linker conjugate (HY-175632)).
    PIK5-12d
  • HY-NP132A
    Recombinant humanized type III collagen (MW 55900)
    		Inhibitor
    Recombinant humanized type III collagen (MW 55900) is a type III collagen with a molecular weight of 55900 Da. Recombinant humanized type III collagen has various biological functions, such as promoting skin extracellular matrix regeneration and improving the cell microenvironment. Recombinant humanized type III collagen inhibits the proliferation, migration, and invasion of breast cancer cells. Type III collagen functions in cell adhesion, migration, proliferation and differentiation through its interaction with integrins.
    Recombinant humanized type III collagen (MW 55900)
  • HY-B0075S1
    Melatonin-d3
    		Inhibitor 99.15%
    Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
    Melatonin-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity
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