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-125848R
    Ginsenoside F2 (Standard)
    		Inducer
    Ginsenoside F2 (Standard) is the analytical standard of Ginsenoside F2. This product is intended for research and analytical applications. Ginsenoside F2, a metabolite from Ginsenoside Rb1, induces apoptosis accompanied by protective autophagy in breast cancer stem cells.
    Ginsenoside F2 (Standard)
  • HY-B0228S3
    Adenosine-3′-13C
    Adenosine-3′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
    Adenosine-3′-<sup>13</sup>C
  • HY-W584517
    Thalidomide-5-O-CH2-COO(t-Bu)
    		Inducer
    Thalidomide-5-O-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-5-O-CH2-COO(t-Bu)
  • HY-173133
    Antitumor agent-199
    		Inducer
    Antitumor agent-199 (Compound 4b) is an antitumor agent. Antitumor agent-199 exhibits significant antiproliferative activity against multiple tumor cell lines. Antitumor agent-199 can induce autophagy in cancer cells via the ATG5/ATG7 pathway and can be used in the study of cancer.
    Antitumor agent-199
  • HY-13955S2
    Telmisartan-13C,d3
    		Inducer
    Telmisartan-13C,d3 is the 13C- and deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan-<sup>13</sup>C,d<sub>3</sub>
  • HY-A0067R
    Oxybenzone (Standard)
    		Inhibitor
    Oxybenzone (Standard) is the analytical standard of Oxybenzone. This product is intended for research and analytical applications. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
    Oxybenzone (Standard)
  • HY-N2593R
    Isorhapontigenin (Standard)
    		Inducer
    Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin. This product is intended for research and analytical applications. Isorhapontigenin, an orally bioavailable dietary polyphenol isolated from the Chinese herb Gnetum cleistostachyum, displays anti-inflammatory effects. Isorhapontigenin induces autophagy and inhibits invasive bladder cancer formation.
    Isorhapontigenin (Standard)
  • HY-12033S
    2-Methoxyestradiol-13C,d3
    		Inducer
    2-Methoxyestradiol-13C,d3 is the 13C- and deuterium labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
    2-Methoxyestradiol-<sup>13</sup>C,d<sub>3</sub>
  • HY-N0281R
    Daphnetin (Standard)
    		Inducer
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin (Standard)
  • HY-203817
    IITZ-02
    		Inhibitor
    IITZ-02 is a lysosomotropic Autophagy inhibitor. IITZ-02 enhances autophagosome accumulation but inhibits autophagosomal degradation by impairing lysosomal function, finally inducing the inhibition of autophagy. IITZ-02 abolishes mitochondrial membrane potential and induces apoptosis through the mitochondria-mediated pathway. IITZ-02 has a potent antitumor activity in MDA-MB-231 xenograft mouse models. IITZ-02 can be used for cancers research.
    IITZ-02
  • HY-N0013R
    Vitexin (Standard)
    Vitexin (Standard) is the analytical standard of Vitexin. This product is intended for research and analytical applications. Vitexin is a c-glycosylated flavone, and is found in various medicinal plants species such as Trigonella foenum-graecum Linn. Vitexin has a wide range of pharmacological effects, including anti-oxidant, anti-cancer, anti-inflammatory, anti-hyperalgesic, and neuroprotective effects.
    Vitexin (Standard)
  • HY-B1287R
    Citalopram hydrobromide (Standard)
    		Inducer
    Citalopram (hydrobromide) (Standard) is the analytical standard of Citalopram (hydrobromide). This product is intended for research and analytical applications. Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect.
    Citalopram hydrobromide (Standard)
  • HY-148255
    QN523
    		Inducer 99.77%
    QN523 is a novel scaffold with agent-like properties, showing potent in vitro cytotoxicity in a panel of 12 cancer cell lines. QN523 induces apoptosis and autophagy. QN523 can be used in research of cancer.
    QN523
  • HY-163193
    MJO445
    MJO445 (Compound 7) is a ATG4B inhibitor, which inhibits the autophagy of glioblastoma.
    MJO445
  • HY-156187
    Anticancer agent 161
    Anticancer agent 161 (Compound 3b) is a bioactive alkynol with anti-cancer potential. Anticancer agent 161 can trigger autophagy and mitochondrial membrane potential depletion.
    Anticancer agent 161
  • HY-156165
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
    		Inducer
    Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
  • HY-N0087R
    Gambogic Acid (Standard)
    		Inducer
    Gambogic Acid (Standard) is the analytical standard of Gambogic Acid. This product is intended for research and analytical applications. Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
    Gambogic Acid (Standard)
  • HY-138849
    Thalidomide-NH-amido-C2-NH2
    		Inducer
    Thalidomide-NH-amido-C2-NH2 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-C2-NH2
  • HY-B1000S
    Selenomethionine-76Se
    Selenomethionine-76Se (Seleno-DL-methionine-76Se) is the 76Se- labeled Selenomethionine (HY-B1000). Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity.
    Selenomethionine-<sup>76</sup>Se
  • HY-178029
    RSK2/TOP2-IN-1
    		Inducer
    RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma.
    RSK2/TOP2-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
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