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-14832S1
    Ataluren-13C6
    Ataluren-13C6 (PTC124-13C6) is 13C labeled Ataluren. Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
    Ataluren-<sup>13</sup>C<sub>6</sub>
  • HY-12053AR
    Vinorelbine ditartrate (Standard)
    		Inducer
    Vinorelbine (ditartrate) (Standard) is the analytical standard of Vinorelbine (ditartrate). This product is intended for research and analytical applications. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
    Vinorelbine ditartrate (Standard)
  • HY-B1490AS3
    Imipramine-d4-1
    		Inducer
    Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). 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.
    Imipramine-d<sub>4</sub>-1
  • HY-B0968S1
    Trimetazidine-d9 dihydrochloride
    		Inducer
    Trimetazidine-d9 (dihydrochloride) is deuterium labeled Trimetazidine (dihydrochloride). Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
    Trimetazidine-d<sub>9</sub> dihydrochloride
  • HY-B0265R
    Nimodipine (Standard)
    		Inducer
    Nimodipine (Standard) is the analytical standard of Nimodipine. This product is intended for research and analytical applications. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders.
    Nimodipine (Standard)
  • HY-N1318R
    Salvigenin (Standard)
    		Inducer
    Salvigenin is a natural polyphenolic compound, with neuroprotective effect. Salvigenin has antitumor cytotoxic and immunomodulatory properties. Salvigenin inhibits H2O2-induced cell apoptosis.
    Salvigenin (Standard)
  • HY-13756S2
    Tacrolimus-d3
    		Inducer
    Tacrolimus-d3 (FK506-d3) is deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
    Tacrolimus-d<sub>3</sub>
  • HY-10328R
    Neflamapimod (Standard)
    Neflamapimod (Standard) is the analytical standard of Neflamapimod (HY-10328). This product is intended for research and analytical applications. Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
    Neflamapimod (Standard)
  • HY-15531S1
    Venetoclax-d6
    		Inducer
    Venetoclax-d6 (ABT-199-d6) is deuterium labeled Venetoclax. Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy.
    Venetoclax-d<sub>6</sub>
  • HY-B0960R
    Sulfabenzamide (Standard)
    		Inducer
    Sulfabenzamide (N-Sulfanilylbenzamide) (Standard) is the analytical standard of Sulfabenzamide (HY-B0960). This product is intended for research and analytical applications. Sulfabenzamide is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
    Sulfabenzamide (Standard)
  • HY-50909R
    Perifosine (Standard)
    		Inducer
    Perifosine (Standard) is the analytical standard of Perifosine. This product is intended for research and analytical applications. Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM.
    Perifosine (Standard)
  • HY-50935R
    Troglitazone (Standard)
    		Inducer
    Troglitazone (Standard) is the analytical standard of Troglitazone. This product is intended for research and analytical applications. Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
    Troglitazone (Standard)
  • HY-N0914R
    Ajugol (Standard)
    		Agonist
    Ajugol (Standard) is the analytical standard of Ajugol (HY-N0914). This product is intended for research and analytical applications. Ajugol is an orally active iridoid glycoside found in the traditional Chinese medicine Leonurus japonicus. Ajugol is an autophagy activator. Ajugol activates TFEB-mediated autophagy and lysosomal biogenesis. Ajugol also has anti-inflammatory effects. Ajugol has great potential in the research of asthma, non-alcoholic fatty liver disease (NAFLD), and osteoarthritis.
    Ajugol (Standard)
  • HY-W727893
    Taurine-15N
    		Inducer
    Taurine-15N (2-Aminoethanesulfonic acid-15N) is 15N labeled Taurine. Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
    Taurine-<sub>15<sub>N<sub>
  • HY-10261BR
    (E/Z)-Afatinib (Standard)
    		Inducer
    (E/Z)-Afatinib (Standard) is the analytical standard of (E/Z)-Afatinib. This product is intended for research and analytical applications. (E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.
    (E/Z)-Afatinib (Standard)
  • HY-15030S1
    Naproxen-d3
    		Inducer 99.14%
    Naproxen-d3 ((S)-Naproxen-d3) is the deuterium labeled Naproxen (HY-15030). Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
    Naproxen-d<sub>3</sub>
  • HY-B2184R
    Sofalcone (Standard)
    Sofalcone (Standard) is the analytical standard of Sofalcone. This product is intended for research and analytical applications. Sofalcone, a gastric antiulcer agent, is known to induce the expression of Heme oxygenase-1 (HO-1) in gastric epithelium.
    Sofalcone (Standard)
  • HY-10963
    Momelotinib mesylate
    		Inhibitor
    Momelotinib mesylate (CYT387 mesylate) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, appr 10-fold selectivity versus JAK3.
    Momelotinib mesylate
  • HY-N10365
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine
    		Activator
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine, a alkaloid, significantly perturbates the features of cellular organelles including early endosomes, mitochondria and autophagosomes (Parkinson’s Disease patient-derived olfactory cells).
    6-(1-Hydroxyethyl)-5,6-dihydrochelerythrine
  • HY-108391R
    C8-Ceramide (Standard)
    		Inducer
    C8-Ceramide (Standard) is the analytical standard of C8-Ceramide (HY-108391). This product is intended for research and analytical applications. C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein Kinase (PKC) in vitro.
    C8-Ceramide (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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