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-10590R
    TWS119 (Standard)
    		Inhibitor
    TWS119 (Standard) is the analytical standard of TWS119. This product is intended for research and analytical applications. TWS119 is a specific inhibitor of GSK-3β, with an IC50 of 30 nM, and activates the wnt/β-catenin pathway.
    TWS119 (Standard)
  • HY-13735E
    Quinacrine methanesulfonate
    		Inhibitor
    Quinacrine (Mepacrine) methanesulfonate is a potent, orally active antimalarial agent with antitumor effects in vitro and in vivo. Quinacrine dihydrochloride inhibits NF-κB and activates p53 signaling, inducing apoptosis in tumor cells.
    Quinacrine methanesulfonate
  • HY-B1392R
    Esmolol hydrochloride (Standard)
    		Inhibitor
    Esmolol hydrochloride (Standard) is the analytical standard of Esmolol hydrochloride (HY-B1392).This product is intended for research and analytical applications. Esmolol hydrochloride is an ultra-short-acting cardioselective β1-adrenergic blocker. Esmolol hydrochloride exerts its antiarrhythmic effect by activating Neurokinin 1 Receptoraldose reductase and the production of advanced glycation end products and promoting fibroblast migration. Esmolol hydrochloride can be used to study cardiac diseases such as arrhythmias and diabetic foot ulcers.
    Esmolol hydrochloride (Standard)
  • HY-N0221R
    Daurisoline (Standard)
    		Inhibitor
    Daurisoline (Standard) is the analytical standard of Daurisoline. This product is intended for research and analytical applications. Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer.
    Daurisoline (Standard)
  • HY-15202S1
    Binimetinib-d3
    		Inhibitor
    Binimetinib-d3 (MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib-d<sub>3</sub>
  • HY-135811AR
    Desethyl chloroquine diphosphate (Standard)
    		Inhibitor
    Desethyl chloroquine (diphosphate) (Standard) is the analytical standard of Desethyl chloroquine (diphosphate). This product is intended for research and analytical applications. Desethyl chloroquine diphosphate is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine diphosphate possesses antiplasmodic activity.
    Desethyl chloroquine diphosphate (Standard)
  • HY-12855
    Lys01
    		Inhibitor
    Lys01, a dimeric form of Chloroquine (HY-17589A), is an autophagy inhibitor. Lys01 inhibits cell viability of 1205Lu, c8161, LN229, HT-29 cells with IC50s of 3.6, 3.8, 7.9, 6.0 μM. Lys01 can be used for anticancer research.
    Lys01
  • HY-100202R
    TPEN (Standard)
    		Inhibitor
    TPEN (Standard) is the analytical standard of TPEN (HY-100202). This product is intended for research and analytical applications. TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn2+, but a lower affinity for Mg2+ and Ca2+. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.
    TPEN (Standard)
  • HY-10402R
    Losmapimod (Standard)
    		Inhibitor
    Losmapimod (Standard) is the analytical standard of Losmapimod. This product is intended for research and analytical applications. Losmapimod (GSK-AHAB) is a selective, potent, and orally active p38 MAPK inhibitor with pKis of 8.1 and 7.6 for p38α and p38β, respectively.
    Losmapimod (Standard)
  • HY-15202R
    Binimetinib (Standard)
    		Inhibitor
    Binimetinib (Standard) is the analytical standard of Binimetinib. This product is intended for research and analytical applications. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib (Standard)
  • HY-W020041
    CP 53631
    		Inhibitor
    CP 53631 is an autophagy inhibitor (Autophagy) with anticancer activity. Additionally, CP 53631 can be used as an internal standard for Sertraline (HY-B0176A) in research related to selective serotonin reuptake inhibitors (SSRIs) in the field of antidepressants .
    CP 53631
  • HY-183732
    ATG5 PPI-IN-2
    		Inhibitor
    ATG5 PPI-IN-2 is a selective inhibitor of ATG5-TECAIR protein-protein interaction, with a IC50 of 19.16 μM. ATG5 PPI-IN-2 also acts as an Autophagy inhibitor.
    ATG5 PPI-IN-2
  • HY-183736
    Autophagy-IN-12
    		Inhibitor
    Autophagy-IN-12 is a Autophagy inhibitor. Autophagy-IN-12 exhibits an IC50 value of >33 μM against the protein-protein interactions of ATG5-ATG16L1 and ATG5-TECAIR.
    Autophagy-IN-12
  • HY-13749D
    (Rac)-Sitagliptin
    		Inhibitor
    (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin
  • HY-B0957R
    Erythromycin Ethylsuccinate (Standard)
    		Inhibitor
    Erythromycin Ethylsuccinate (Standard) is the analytical standard of Erythromycin Ethylsuccinate. This product is intended for research and analytical applications. Erythromycin Ethylsuccinate is an antibiotic useful for the treatment of a number of bacterial infections, has an antimicrobial spectrum similar to or slightly wider than that of penicillin. Erythromycin Ethylsuccinate has antiviral activity against HIV-1.
    Erythromycin Ethylsuccinate (Standard)
  • HY-N0484R
    Liensinine (Standard)
    		Inhibitor
    Liensinine (Standard) is the analytical standard of Liensinine (HY-N0484). This product is intended for research and analytical applications. Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.
    Liensinine (Standard)
  • HY-13418R
    Dorsomorphin dihydrochloride (Standard)
    		Inhibitor
    Dorsomorphin (dihydrochloride) (Standard) is the analytical standard of Dorsomorphin (dihydrochloride). This product is intended for research and analytical applications. Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
    Dorsomorphin dihydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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