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-101273
    BAR502
    		99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-B1417S
    Nortriptyline-d3 hydrochloride
    		Inducer 99.75%
    Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression[1].
    Nortriptyline-d<sub>3</sub> hydrochloride
  • HY-169369
    TRAP-1
    		99.69%
    TRAP-1 (XJZ-06-462) is ap53 transcriptional activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. TRAP-1 rapidly upregulates p21 and other p53 target genes in pancreatic cell lines with p53Y220C. TRAP-1 inhibits cell proliferation, with IC50 values of 3.94 and 0.531 μM in BxPC-3 and A549 cells, respectively. TRAP-1 regulates autophagy in lung cancer cells and offers protective effects against oxidative stress and cell apoptosis.
    TRAP-1
  • HY-B0715S2
    Pentoxifylline-d5
    		Inducer 99.86%
    Pentoxifylline-d5 is the deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation[1][2][3].
    Pentoxifylline-d<sub>5</sub>
  • HY-NP131
    Recombinant Humanized Type III Collagen (10.4kDa)
    		Inhibitor
    Recombinant Humanized Type III Collagen 10.4kDa is a novel biomaterial that have anticancer effects. Recombinant Humanized Type III Collagen 10.4kDa activates discoidin domain receptor 1 (DDR1), and thus inhibits autophagy, proliferation, and migration of cancer cells, and induces apoptosis.
    Recombinant Humanized Type III Collagen (10.4kDa)
  • HY-B1756R
    Rotenone (Standard)
    		Inhibitor
    Rotenone (Standard) is the analytical standard of Rotenone. This product is intended for research and analytical applications. Rotenone is a mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
    Rotenone (Standard)
  • HY-B1203AR
    Fludrocortisone acetate (Standard)
    		Inducer 98.77%
    Fludrocortisone acetate (Standard) is the analytical standard of Fludrocortisone acetate. This product is intended for research and analytical applications.
    Fludrocortisone acetate (Standard)
  • HY-W457950
    Thalidomide-5-propargyl
    		Inducer
    Thalidomide-5-propargyl is a propargyl-modified Thalidomide (HY-14658), that acts as a Cereblon ligand to recruit CRBN proteins. Thalidomide-5-propargyl use alkynyl group at the end to be directly used in the synthesis of triazoles in the synthesis of PROTAC molecules, and is a key intermediate in the synthesis of PROTAC molecules based on CRBN design.
    Thalidomide-5-propargyl
  • HY-B0965AS
    Thioridazine-d3 hydrochloride
    		Inducer 99.19%
    Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs)[1][2][3][4].
    Thioridazine-d<sub>3</sub> hydrochloride
  • HY-148556
    Thalidomide-O-C6-azide
    		Inducer 99.71%
    Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate (E3 Ligase Ligand-Linker Conjugates) that incorporates the Thalidomide (Thalidomide (HY-14658)) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C6-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Thalidomide-O-C6-azide
  • HY-15654S
    Phenylbutyrate-d11 sodium
    		Inducer 99.85%
    Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research[1].
    Phenylbutyrate-d<sub>11</sub> sodium
  • HY-103704
    LY2562175
    		99.49%
    LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
    LY2562175
  • HY-17514S2
    Itraconazole-d9
    Itraconazole-d9 is the deuterium labeled Itraconazole[1]. Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor[2][3][4][5].
    Itraconazole-d<sub>9</sub>
  • HY-W344044
    Levomepromazine maleate
    		Inducer 99.92%
    Levomepromazine maleate (Methotrimeprazine maleate) is an N-substituted phenylthiazine antipsychotic sedative that blocks multiple receptors. Levomepromazine maleate is a potent inhibitor of CYP2D6 and is useful in the study of schizophreni.
    Levomepromazine maleate
  • HY-136540
    Resolvin D3
    Resolvin D3 (RvD3) is a docosahexaenoic acid (DHA) derived mediator. Resolvin D3 is dysregulated in arthritis and reduces arthritic inflammation.
    Resolvin D3
  • HY-76847S2
    Chenodeoxycholic acid-13C
    		≥98.0%
    Chenodeoxycholic acid-13C is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-<sup>13</sup>C
  • HY-15463S2
    Imatinib-d3 hydrochloride
    Imatinib-d3 (hydrochloride) is the deuterium labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-d<sub>3</sub> hydrochloride
  • HY-N0384R
    Homovanillic acid (Standard)
    		Inhibitor
    Homovanillic acid (Standard) is the analytical standard of Homovanillic acid. This product is intended for research and analytical applications. Homovanillic acid is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
    Homovanillic acid (Standard)
  • HY-B0015S1
    Paclitaxel-d5 (benzoyloxy)
    		Inducer 98.12%
    Paclitaxel-d5 (benzoyloxy) is the deuterium labeled Paclitaxel. Paclitaxel is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Paclitaxel also induces autophagy[1][2].
    Paclitaxel-d<sub>5</sub> (benzoyloxy)
  • HY-161872
    LC3in-C42
    		Inhibitor
    LC3in-C42 is a cell-active LC3A/B and autophagy covalent inhibitor. LC3in-C42 selectively inhibits the binding of P62 to LC3A/B in vitro and at the cellular level like D5 and can function on a lower concentration.
    LC3in-C42
Cat. No. Product Name / Synonyms Application Reactivity
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