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-75839
    Dronedarone Hydrochloride
    		Inducer 99.99%
    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
    Dronedarone Hydrochloride
  • HY-10562A
    Ketanserin tartrate
    		Inducer 99.99%
    Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
    Ketanserin tartrate
  • HY-N0017
    Bergenin
    		Inhibitor 99.21%
    Bergenin is a cytoprotective and antioxidative polyphenol found in many medicinal plants. Bergenin has a wide spectrum activities such as hepatoprotective, antiinflammatory, immunomodulatory, antitumor, antiviral, and antifungal properties.
    Bergenin
  • HY-10214
    SNX-2112
    		Inducer 99.49%
    SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively.
    SNX-2112
  • HY-134050
    Apostatin-1
    		Inducer 99.84%
    Apostatin-1 (Apt-1) is a potent TRADD inhibitor. Apostatin-1 can bind with TRADD-N (KD=2.17 μM), disrupting its binding to both TRADD-C and TRAF2. Apostatin-1 modulates the ubiquitination of RIPK1 and beclin 1. Apostatin-1 blocks apoptosis and restores cellular homeostasis by activating autophagy in cells with accumulated mutant tau, α-synuclein, or huntingtin.
    Apostatin-1
  • HY-N1441
    Afzelin
    		Inhibitor 99.62%
    Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.
    Afzelin
  • HY-W018791
    Bifendate
    		Inhibitor 99.91%
    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
  • HY-W011209
    N6-Isopentenyladenosine
    		Inhibitor 99.66%
    N6-Isopentenyladenosine (Riboprine), an RNA modification found in cytokinins, which regulate plant growth/differentiation, and a subset of tRNAs, where it improves the efficiency and accuracy of translation. N6-Isopentenyladenosine, an end product of the mevalonate pathway, is an autophagy inhibitor with an interesting anti-melanoma activity.
    N6-Isopentenyladenosine
  • HY-N0399
    Wogonoside
    		Inducer 99.91%
    Wogonoside, a flavonoid glycoside isolated from Huangqin, possesses anti-inflammatory effects. Wogonoside induces autophagy in breast cancer cells by regulating MAPK-mTOR pathway.
    Wogonoside
  • HY-N0783
    Eupatilin
    		Inducer 98.90%
    Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi Lévl. et Van., is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
    Eupatilin
  • HY-13287
    SGI-1776 free base
    		Inducer 99.35%
    SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
    SGI-1776 free base
  • HY-76847S
    Chenodeoxycholic Acid-d4
    		99.53%
    Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>4</sub>
  • HY-139426A
    (rel)-ML-SI3
    		Inducer 98.94%
    (rel)-ML-SI3 is one of the active ingredients of ML-SI3 (HY-139426) (another component is (cis)-ML-SI3) that targets three isoforms of TRPML. (rel)-ML-SI3 is an inhibitor of TRPML1 and TRPML3 (IC50=3.1 μM/28.5 μM), and a potent activator of TRPML2 (EC50=3.3 μM).
    (rel)-ML-SI3
  • HY-17386A
    Rosiglitazone hydrochloride
    		Inducer 99.81%
    Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC50: 60 nM, Kd: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC50: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.
    Rosiglitazone hydrochloride
  • HY-N0289
    Lycorine hydrochloride
    		Inhibitor 99.89%
    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
  • HY-10248
    RAF265
    		Inducer 99.80%
    RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265
  • HY-136351
    THZ-P1-2
    		Inhibitor 99.86%
    THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
    THZ-P1-2
  • HY-N0837
    Veratramine
    		Inducer 99.84%
    Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy.
    Veratramine
  • HY-134832
    Mito-LND
    		Inducer
    Mito-LND (Mito-Lonidamine) is an orally active and mitochondria-targeted inhibitor of oxidative phosphorylation (OXPHOS). Mito-LND inhibits mitochondrial bioenergetics, stimulates the formation of reactive oxygen species, and induces autophagic cell death in lung cancer cells.
    Mito-LND
  • HY-129960
    L-Selenocystine
    		Inhibitor
    L-Selenocystine is a selenium-containing amino acid. L-Selenocystine has redox properties. L-Selenocystine is cytotoxic to various tumor cells and can induce the production of ROS and apoptosis. L-Selenocystine can block the Nrf2 and autophagy pathways. L-Selenocystine has anti-tumor activity.
    L-Selenocystine
Cat. No. Product Name / Synonyms Application Reactivity
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