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-B0075S2
    Melatonin-d7
    		Inhibitor 98.85%
    Melatonin-d7 is the deuterium labeled Melatonin (HY-B0075). Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
    Melatonin-d<sub>7</sub>
  • HY-13676R
    Megestrol acetate (Standard)
    		Inhibitor
    Megestrol acetate (Standard) is the analytical standard of Megestrol acetate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-156966
    ATG12-ATG3 inhibitor 1
    		Inhibitor 98.19%
    ATG12-ATG3 inhibitor 1 (compound 189) is a potent inhibitor of autophage.
    ATG12-ATG3 inhibitor 1
  • HY-N2282
    Zingiberen newsaponin
    		Inhibitor 99.68%
    Zingiberen Newsaponin (Zingiberensis newsaponin) is an orally active type of steroid saponin compound. Zingiberen Newsaponin exerts anti-hepatocellular carcinoma (HCC) effects by inhibiting autophagy and the AKR1C1/JAK2/STAT3 pathway. Zingiberen Newsaponin activates oxidative stress (upregulates ROS and MDA) and mitochondrial pathways, promoting cancer cell apoptosis. Zingiberen Newsaponin alleviates cerebral ischemia-reperfusion (I/R) injury by decreasing the concentration of pro-inflammatory cytokines and inhibits NF-κB. Zingiberen Newsaponin can enhance the activity of SOD, eliminate free radicals and protect nerve cells. Zingiberen Newsaponin induces platelet aggregation.
    Zingiberen newsaponin
  • HY-N0485
    Liensinine Diperchlorate
    		Inhibitor 99.96%
    Liensinine Diperchlor​ate is a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn. Liensinine Diperchlor​ate inhibits late-stage autophagy/mitophagy through blocking autophagosome-lysosome fusion. Liensinine Diperchlor​ate has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
    Liensinine Diperchlorate
  • HY-14393R
    Emodin (Standard)
    		Inhibitor
    Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
    Emodin (Standard)
  • HY-15758R
    3,3'-Diindolylmethane (Standard)
    		Inhibitor
    3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
    3,3'-Diindolylmethane (Standard)
  • HY-119357
    TN-16
    		Inhibitor 99.78%
    TN-16 is a Microtubule polymerization inhibitor. TN-16 induces G2/M cell cycle arrest, metaphase mitotic arrest and Apoptotic cell death in cells, and blocks late Autophagic flux by inhibiting autophagosome-lysosome fusion. TN-16 suppresses tumor growth in syngeneic mouse breast cancer models. TN-16 can be used in research related to neuroblastoma, cervical cancer, breast cancer and other tumors.
    TN-16
  • HY-176835
    PNR-3-80
    		Inhibitor 98.63%
    PNR-3-80 is an endonuclease G (ENDOG) inhibitor with an IC50 of 0.67 μM. As a non-competitive binder to the ENDOG-substrate complex, PNR-3-80 specifically inhibits the endonuclease activity of ENDOG. PNR-3-80 reduces cell death induced by Cisplatin (HY-17394) and Docetaxel (HY-B0011), and inhibits DNA damage and autophagy (autophagy) induced by Etoposide (HY-13629). PNR-3-80 can be used in studies related to cell injury.
    PNR-3-80
  • HY-136068
    DCAP
    		Inhibitor 99.0%
    DCAP is a broad-spectrum antibiotic targeting the membranes of both Gram-positive and Gram-negative bacteria. DCAP blocks autophagy at the late stages by preventing autophagolysosome maturation and interrupting the autophagic flux.
    DCAP
  • HY-15184
    Elaiophylin
    		Inhibitor 98.0%
    Elaiophylin (Azalomycin B; Gopalamicin; Efomycin E) is an autophagy inhibitor, exerts antitumor activity as a single agent in ovarian cancer cells.
    Elaiophylin
  • HY-135811A
    Desethyl chloroquine diphosphate
    		Inhibitor 99.72%
    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
  • HY-112711
    LV-320
    		Inhibitor
    LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 μM and a Kd of 16 μM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo.
    LV-320
  • HY-176954
    RSC-1255
    		Inhibitor 99.91%
    RSC-1255 is a potent and selective Vacuolar H⁺-ATPase (V-ATPase) inhibitor that directly binds the mammalian V-ATPase complex with a Kd = 23 nM. RSC-1255 exhibits preferential cytotoxicity toward KRAS-mutant cancer cells, especially KRASG13D and KRASG12V cells. RSC-1255 induces apoptosis and blocks lysosomal acidification, autophagy, and macropinocytosis in cancer cells. RSC-1255 can be used for the study of KRAS-driven lung and colon cancers.
    RSC-1255
  • HY-B0957
    Erythromycin Ethylsuccinate
    		Inhibitor
    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
  • HY-B0642R
    Isosorbide mononitrate (Standard)
    		Inhibitor
    Isosorbide mononitrate (Standard) is the analytical standard of Isosorbide mononitrate. This product is intended for research and analytical applications. Isosorbide mononitrate (Isosorbide-5-mononitrate) is a nitric acid compound used for angina pectoris by dilating blood vessels and lowering blood pressure.
    Isosorbide mononitrate (Standard)
  • HY-134807
    Indophagolin
    		Inhibitor 98.05%
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
    Indophagolin
  • HY-B0803S1
    Lumefantrine-d9
    		Inhibitor
    Lumefantrine-d9 is the deuterium labeled Lumefantrine. Lumefantrine is an antimalarial drug, used in combination with Artemether. The artemether-lumefantrine (AL) as the first- and second-line anti-malarial drugs.
    Lumefantrine-d<sub>9</sub>
  • HY-N0136R
    Taxifolin (Standard)
    		Inhibitor
    Taxifolin (Standard) is the analytical standard of Taxifolin. This product is intended for research and analytical applications. 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 (Standard)
  • HY-W008581
    Estradiol 3-methyl ether
    		Inhibitor 99.07%
    Estradiol 3-methyl ether (EDME) is a highly selective TRPML1 ion channel antagonist and microtubule (microtubule) depolymerizing agent, with IC50 values of 0.22 μM and 3.8 μM against TRPML1 and TRPML2, respectively; it shows no activity against TRPML3. Estradiol 3-methyl ether induces the disruption of cytoplasmic microtubule networks in mammalian cells, with an EC50 of 9 μM. Independent of estrogen receptors, Estradiol 3-methyl ether blocks autophagy (autophagy), TFEB nuclear translocation, and inhibits the migration and invasion of triple-negative breast cancer cells by suppressing TRPML1. Estradiol 3-methyl ether is applicable for relevant research on triple-negative breast cancer.
    Estradiol 3-methyl ether
Cat. No. Product Name / Synonyms Application Reactivity
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