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-W018791R
    Bifendate (Standard)
    		Inhibitor
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).
    Bifendate (Standard)
  • HY-N0221S
    Daurisoline-d2
    		Inhibitor
    Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). 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-d<sub>2</sub>
  • HY-169592
    Autophagy-IN-7
    		Inhibitor
    Autophagy-IN-7 is an autophagy inhibitor that can be used in the study of cancer.
    Autophagy-IN-7
  • HY-17437R
    Mefloquine (Standard)
    		Inhibitor
    Mefloquine (Standard) is the analytical standard of Mefloquine. This product is intended for research and analytical applications. Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K+ channel (KvQT1/minK) antagonist with an IC50 of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.
    Mefloquine (Standard)
  • HY-101971R
    AZ PFKFB3 26 (Standard)
    		Inhibitor
    AZ PFKFB3 26 (Standard) is the analytical standard of AZ PFKFB3 26 (HY-101971). This product is intended for research and analytical applications. AZ PFKFB3 26 is a potent and selective PFKFB3 inhibitor with an IC50 of 23 nM. AZ PFKFB3 26 inhibits PFKFB1 and PFKFB2 with IC50s of 2.06 and 0.384 μM, respectively. AZ PFKFB3 26 can be used in the study of non-small cell lung cancer.
    AZ PFKFB3 26 (Standard)
  • HY-N0589R
    Dehydrodiisoeugenol (Standard)
    		Inhibitor
    Dehydrodiisoeugenol (Standard) is the analytical standard of Dehydrodiisoeugenol (HY-N0589). This product is intended for research and analytical applications. Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol (Standard)
  • HY-N0221S2
    Daurisoline-d11
    		Inhibitor
    Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). 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-d<sub>11</sub>
  • HY-10231R
    PX-478 (Standard)
    		Inhibitor
    PX-478 (Standard) is the analytical standard of PX-478 (HY-10231). This product is intended for research and analytical applications. PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
    PX-478 (Standard)
  • HY-12075R
    LY2109761 (Standard)
    		Inhibitor
    LY2109761 (Standard) is the analytical standard of LY2109761. This product is intended for research and analytical applications. LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
    LY2109761 (Standard)
  • HY-17507S2
    Pantoprazole-d8
    		Inhibitor
    Pantoprazole-d8 (BY1023-d8) is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
    Pantoprazole-d<sub>8</sub>
  • HY-15431R
    Capivasertib (Standard)
    		Inhibitor
    Capivasertib (Standard) is the analytical standard of Capivasertib. This product is intended for research and analytical applications. Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.
    Capivasertib (Standard)
  • HY-111159
    CP-467688
    		Inhibitor
    CP-467688 is an orally active retinotoxic agent. CP-467688 induces increased lysosome volume, phagocytosis inhibition and autophagy inhibition in retinal cells. CP-467688 is applicable to the research of retinopathy.
    CP-467688
  • HY-15202S3
    Binimetinib-d4
    		Inhibitor
    Binimetinib-d4 (MEK162-d4) 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>4</sub>
  • HY-103706R
    ROC-325 (Standard)
    		Inhibitor
    ROC-325 (Standard) is the analytical standard of ROC-325 (HY-103706). This product is intended for research and analytical applications. ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
    ROC-325 (Standard)
  • HY-13735BR
    Quinacrine hydrochloride hydrate (Standard)
    		Inhibitor
    Quinacrine (hydrochloride hydrate) (Standard) is the analytical standard of Quinacrine (hydrochloride hydrate). This product is intended for research and analytical applications. Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
    Quinacrine hydrochloride hydrate (Standard)
  • HY-160475
    AD-9308
    		Inhibitor
    AD-9308 is a highly selective and orally active ALDH2 activator. AD-9308 activates ALDH2 to promote the clearance of 4-HNE, inhibiting myocardial fibrosis, inflammation and cell apoptosis. AD-9308 improves mitochondrial function, sarcoplasmic reticulum/ endoplasmic reticulum calcium transport and regulates autophagy, restoring intracellular homeostasis. AD-9308 improves the diastolic and systolic function of the heart in diabetic mice and reverses ventricular mal-reconstruction. AD-9308 can be used for the study of diabetic cardiomyopathy.
    AD-9308
  • HY-W777418
    Isosorbide mononitrate-13C6
    		Inhibitor
    Isosorbide mononitrate-13C6 (Isosorbide-5-mononitrate-13C6) is 13C-labeled Isosorbide mononitrate (HY-B0642).
    Isosorbide mononitrate-<sup>13</sup>C<sub>6</sub>
  • HY-A0077R
    Perphenazine (Standard)
    		Inhibitor
    Perphenazine (Standard) is the analytical standard of Perphenazine. This product is intended for research and analytical applications. Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
    Perphenazine (Standard)
  • HY-132489S
    (Rac)-Sitagliptin-d4
    		Inhibitor
    (Rac)-Sitagliptin-d4 ((Rac)-MK-0431-d4) is the deuterium labeled (Rac)-Sitagliptin. (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-d<sub>4</sub>
  • HY-112903A
    YW3-56 hydrochloride
    		Inhibitor
    YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer.
    YW3-56 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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