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-111287
    Autophagonizer
    		Inducer
    Autophagonizer (DK-1-49) is a small molecule autophagy inducer that results in an accumulation of autophagy-associated LC3-II and enhances levels of autophagosomes and acidic vacuoles. Autophagonizer inhibits cell viability and induces cell death in not only cancer cells but also Bax/Bak double-knockout cells with EC50 values of 3-4 μM.
    Autophagonizer
  • HY-162344
    Ir-CA
    		Inducer
    Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9.
    Ir-CA
  • HY-163136A
    Autophagy/REV-ERB-IN-1 hydrochloride
    		Inhibitor
    Autophagy/REV-ERB-IN-1 hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved potency in blocking autophagy, enhanced toxicity against cancer cells. Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for melanoma.
    Autophagy/REV-ERB-IN-1 hydrochloride
  • HY-149575
    Thalidomide-4-O-C13-NH2 hydrochloride
    		Inducer 99.75%
    Thalidomide-4-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C13-NH2 hydrochloride
  • HY-B1227S
    Carprofen-d3
    Carprofen-d3 is the deuterium labeled Carprofen. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
    Carprofen-d<sub>3</sub>
  • HY-118032
    Bozepinib
    		Inducer
    Bozepinib is a PKR (RNA-dependent protein kinase) activator and potently inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces PKR-mediated apoptosis and synergizes with IFNα to trigger apoptosis, autophagy and senescence. Bozepinib also demonstrates in vivo antitumor and antimetastatic efficacy in xenografted nude mice.
    Bozepinib
  • HY-B1756S
    Rotenone-d3
    		Inhibitor
    Rotenone-d3 is the deuterium labeled Rotenone (HY-B1756). Rotenone is a mitochondrial electron transport chain complex I inhibitor. Rotenone induces apoptosis through enhancing mitochondrial reactive oxygen species production.
    Rotenone-d<sub>3</sub>
  • HY-10331AR
    Regorafenib monohydrate (Standard)
    		Inducer
    Regorafenib (monohydrate) (Standard) is the analytical standard of Regorafenib (monohydrate). This product is intended for research and analytical applications. Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.
    Regorafenib monohydrate (Standard)
  • 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-158288
    Pyrazinamide-BSA
    		Inducer
    Pyrazinamide-BSA is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Pyrazinamide-BSA
  • HY-162365
    JD-02
    		Inducer
    JD-02 is a novel Hsp90 inhibitor. JD-02 can induce autophagy and apoptosis. JD-02 increses the level of reactive oxygen species.
    JD-02
  • 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-161204
    Thalidomide-O-C4H4-N(Me)-piperidine-boc
    		Inducer
    Thalidomide-O-C4H4-N(Me)-piperidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-piperidine-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-O-C4H4-N(Me)-piperidine-boc
  • HY-144637
    Autophagy inducer 2
    Autophagy inducer 2 (Compound 11i) is a potent autophagy inducer. Autophagy inducer 2 exhibits apparent antiproliferative activity against the MCF-7 cell line with an IC50 value of 1.31 μM and remarkably inhibits the colony formation of the MCF-7 cells. Autophagy inducer 2 arrests the MCF-7 cells in the G2/M phase by regulating the cell-cycle-related proteins Cdk-1 and Cyclin B1. Autophagy inducer 2 has the potential for the research of breast cancer.
    Autophagy inducer 2
  • HY-138855A
    Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-PEG2-C2-NH2 hydrochloride
  • HY-P10711
    ALA-A2 peptide
    ALA-A2 is an anticancer peptide discovered in alpha-lactalbumin that selectively kills cancer cells by inducing Autophagy. ALA-A2 has cell-penetrating capabilities, allowing it to effectively enter cells without relying on membranolytic effects. In A549 lung cancer cells, ALA-A2 demonstrates significant dose-dependent anticancer activity. ALA-A2 holds promise for research in cancer therapy and autophagy regulation.
    ALA-A2 peptide
  • HY-100490S
    Rilmenidine-d4
    		Inducer
    Rilmenidine-d4 is the deuterium labeled Rilmenidine. Rilmenidine, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine is an alpha 2-adrenoceptor agonist. Rilmenidine induces autophagy. Rilmenidine acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells.
    Rilmenidine-d<sub>4</sub>
  • HY-160902
    2G-HaloAUTAC
    		Inducer
    2G-HaloAUTAC (Compound tt44) is a Autophagy-targeting chimera (2G-HaloAUTAC) that improves the activity of AUTACs by replacing the L-Cysteine ​​(L-Cys) linker with other structures. 2G-HaloAUTAC exhibits degradation activity against EGFP-HaloTag protein through an Autophagic mechanism.
    2G-HaloAUTAC
  • 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-13067G
    Celastrol (GMP)
    		Inducer
    Celastrol (GMP) (Tripterine (GMP)) is Celastrol (HY-10227) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
    Celastrol (GMP)
Cat. No. Product Name / Synonyms Application Reactivity
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