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-162932
    ATG12-IN-1
    		Inhibitor
    ATG12-IN-1 (compound 4) is an autophagy inhibitor (IC50=9 μM) targeting the ATG12-ATG3 protein-protein interaction, which can be used in cancer research.
    ATG12-IN-1
  • HY-N0136S
    Taxifolin-d3
    		Inhibitor
    Taxifolin-d3 is deuterium labeled Taxifolin. Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
    Taxifolin-d<sub>3</sub>
  • HY-13676S1
    Megestrol acetate-d3-1
    		Inhibitor
    Megestrol acetate-d3-1 is deuterium labeled Megestrol acetate. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
    Megestrol acetate-d<sub>3</sub>-1
  • HY-135811
    Desethyl chloroquine
    		Inhibitor
    Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.
    Desethyl chloroquine
  • HY-W550739
    Acesulfame
    		Inhibitor
    Acesulfame is a synthetic sweetener. Long-term use of Acesulfame can affect cognitive function. Acesulfame potassium can suppress autophagic degradation of PD-L1 in RIL-175 and SK-Hep1 cells through the ERK1/2-mTORC1-ULK1 pathway, which may be related to immune evasion in cancer cells. Acesulfame can be used in research on neurological diseases, metabolic disorders, cancer, and immune evasion.
    Acesulfame
  • HY-17589S
    Chloroquine-d5 diphosphate
    		Inhibitor
    Chloroquine-d5 (diphosphate) is the deuterium labeled Chloroquine (phosphate). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine-d<sub>5</sub> diphosphate
  • HY-150757
    Autophagy-IN-2
    		Inhibitor
    Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research.
    Autophagy-IN-2
  • HY-124132
    Autophagy-IN-4
    		Inhibitor 99.35%
    Autophagy-IN-4 (Compound 34) is an autophagy inhibitor, with an EC50 of 0.5 μM and a LD50 of 27 μM for U2OS cells.
    Autophagy-IN-4
  • HY-149829
    Antitumor agent-97
    		Inhibitor
    Antitumor agent-97 (compound 42) is an anticancer agent. Antitumor agent-97 can effectively inhibit the proliferation and autophagy of MGC 803 cells, and induce apoptosis. Antitumor agent-97 also enhances ROS accumulation in MGC 803 cells. Antitumor agent-97 can be used in cancer research.
    Antitumor agent-97
  • HY-116071
    Autophagy-IN-3
    		Inhibitor
    Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments.
    Autophagy-IN-3
  • HY-170670
    DQ661
    		Inhibitor
    DQ661 is a potent PPT1 inhibitor. DQ661 is a dimeric quinacrine autophagy inhibitor. DQ661 inhibits mTORC1 activity. DQ661 decreases the protein expression of pS6K T389, pS6 S240-244. DQ661 shows anticancer activity.
    DQ661
  • HY-161850
    ULK1-IN-3
    		Inhibitor
    ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.
    ULK1-IN-3
  • HY-132885
    PARP/EZH2-IN-1
    		Inhibitor
    PARP/EZH2-IN-1 is a first-in-class dual PARP-1/EZH2 inhibitor with IC50 values of 6.87 nM and 36.51 nM, respectively. PARP/EZH2-IN-1 induces autophagy in cancer cells and shows potent antiproliferative activity in BRCA wild-type triple-negative breast cancer cells.
    PARP/EZH2-IN-1
  • HY-163136
    Autophagy/REV-ERB-IN-1
    		Inhibitor
    Autophagy/REV-ERB-IN-1 (compound 24) is a dual inhibitor of autophagy and REV-ERB. Autophagy/REV-ERB-IN-1 has anti-tumor activity with a CC50 value of 2.3 μM on BTB-474 cells.
    Autophagy/REV-ERB-IN-1
  • HY-156348
    MAO-B-IN-26
    		Inhibitor
    MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease.
    MAO-B-IN-26
  • HY-B0532S
    Trifluoperazine-d8
    		Inhibitor
    Trifluoperazine-d8 is a deuterium labeled Trifluoperazine. Trifluoperazine is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor .
    Trifluoperazine-d<sub>8</sub>
  • HY-183867
    ATG5 PPI-IN-6
    		Inhibitor
    ATG5 PPI-IN-6 is an inhibitor of ATG5 interactions with other proteins, with an IC50 value of 26.92 μM against ATG5-ATG16L1 and 16.34 μM against ATG5-TECAIR. ATG5 PPI-IN-6 inhibits Autophagy in cells.
    ATG5 PPI-IN-6
  • HY-183807
    T1742
    		Inhibitor
    T1742 is an autophagy inhibitor targeting ATG5. T1742 blocks and disrupts protein-protein interactions between ATG5 and ATG16L1, and between ATG5 and TECAIR.T 1742 inhibits autophagy in living cells via reduced autophagosome formation and downregulated ATG8-PE conjugation. T1742 can be used to study autophagy mechanisms.
    T1742
  • HY-N0289R
    Lycorine hydrochloride (Standard)
    		Inhibitor
    Lycorine (hydrochloride) (Standard) is the analytical standard of Lycorine (hydrochloride). This product is intended for research and analytical applications. Lycorine hydrochloride is the main active ingredient of the herbal medicine derived from Lycoris radiata (L’Her.) Herb. and is also a melanoma vasculogenic inhibitor and has anti-tumor activity. Lycorine hydrochloride effectively inhibits mitotic proliferation of Hey1B cells (IC50 of 1.2 μM).
    Lycorine hydrochloride (Standard)
  • HY-183838
    Autophagy-IN-11
    		Inhibitor
    Autophagy-IN-11 is an ATG5-targeting autophage inhibitor. Autophagy-IN-11 disrupts protein-protein interactions between ATG5 and ATG16L1, and between ATG5 and TECAIR. Autophagy-IN-11 can be used for cancer research.
    Autophagy-IN-11
Cat. No. Product Name / Synonyms Application Reactivity
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