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-173331
    Antitumor agent-201
    		Inducer
    Antitumor agent-201 (Compound 10) is a chloride transport activator that targets the Golgi apparatus. Its EC50 for promoting the transmembrane transport of chloride ions is 1.53 mol%, and its IC50 against HepG2 cells is 7.13 μM. Antitumor agent-201 exerts its anti-cancer activity by selectively acting on the Golgi apparatus, disrupting the chloride ion homeostasis within it, reducing the expression of key proteins such as GM130 and GRASP55, altering the structure and function of the Golgi apparatus, triggering Autophagy of the Golgi apparatus, and further inducing Apoptosis of cancer cells and arresting cancer cells in the G2/M phase. Antitumor agent-201 can be used in the research field of cancer diseases.
    Antitumor agent-201
  • HY-W584524
    Thalidomide-4-NH-PEG2-COO(t-Bu)
    		Inducer
    Thalidomide-4-NH-PEG2-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-4-NH-PEG2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG2-COO(t-Bu)
  • HY-176749
    HUP-46
    		Activator
    HUP-46 is a BBB-penatrable modulator of αSyn dimerization and autophagy. HUP-46 reduces the ratio of pPP2A/PP2A, increases the autophagy marker LC3BII levels, and decreases αSyn dimerization. HUP-46 can be used for research of neurodegenerative diseases.
    HUP-46
  • HY-N0716BR
    Berberine sulfate (Standard)
    		Modulator
    Berberine (sulfate) (Standard) is the analytical standard of Berberine (sulfate). This product is intended for research and analytical applications. Berberine sulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine sulfate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine sulfate has antineoplastic properties. The sulfate form improves bioavailability[1][2].
    Berberine sulfate (Standard)
  • HY-166562S
    Levomepromazine-d6 hydrochloride
    		Inducer
    Levomepromazine-d6 hydrochloride (Methotrimeprazine-d6 hydrochloride) is the deuterium labeled Levomepromazine hydrochloride. Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting.
    Levomepromazine-d<sub>6</sub> hydrochloride
  • HY-W653958
    Oxybenzone-d3
    Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium labeled Oxybenzone (HY-A0067). 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-d<sub>3</sub>
  • HY-139062
    C6 Urea Ceramide
    		Inducer
    C6 Urea Ceramide (Cer(d18:1/6:0) Urea) is an inhibitor of neutral ceramidase. C6 Urea Ceramide increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and HT-29 colon cancer cells. C6 Urea Ceramide (5-10 μM) inhibits proliferation of HT-29 cells and induces apoptosis and autophagy, but is not toxic to non-cancerous cells. C6 Urea Ceramide decreases total and phosphorylated β-catenin levels in HT-29 and HCT116 cells, and induces colocalization of β-catenin with the 20S proteasome. C6 Urea Ceramide (1.25, 2.5, and 5 mg/kg) reduced tumor growth and increased C16, C18, C20, and C24 ceramide levels in tumor tissues in the HT-29 mouse xenograft model.
    C6 Urea Ceramide
  • HY-B0146R
    Verteporfin (Standard)
    		Inhibitor
    Verteporfin (Standard) is the analytical standard of Verteporfin. This product is intended for research and analytical applications. Verteporfin (CL 318952) is a photosensitizer for photodynamic therapy to eliminate the abnormal blood vessels in the eye associated with conditions such as age-related macular degeneration. Verteporfin is a YAP inhibitor which disrupts YAP-TEAD interactions. Verteporfin induces cell apoptosis. Verteporfinis an autophagy inhibitor that blocks autophagy at an early stage by inhibiting autophagosome formation.
    Verteporfin (Standard)
  • HY-N0504S1
    Lovastatin-d9 (epimer mixture)
    		99.04%
    Lovastatin-d9 is the deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Lovastatin-d<sub>9</sub> (epimer mixture)
  • HY-10224S
    Panobinostat-d4
    		Inducer
    Panobinostat-d4 is the deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
    Panobinostat-d<sub>4</sub>
  • HY-120325
    DHMPA
    		Inducer
    DHMPA is an effective depletor of norepinephrine content of the heart, brain and spleen in mouse and rat. DHMPA has antihypertensive effects.
    DHMPA
  • HY-D3005
    NpCy-4
    NpCy-4 is a reliable reporter for monitoring lysosomal pH and viscosity changes in real time during Autophagy (λex = 650 nm; λem = 660-740 nm). NpCy-4 demonstrates a superior signal-to-background ratio (SBR) for cellular imaging. NpCy-4 facilitates real-time, noninvasive diagnostic imaging of acute gastritis model with high contrast.
    NpCy-4
  • HY-156171
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
    		Inducer
    Thalidomide-5-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
  • HY-B0165AS
    Pravastatin-13C,d3 sodium
    Pravastatin-13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin-<sup>13</sup>C,d<sub>3</sub> sodium
  • HY-161198
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc
    		Inducer
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc
  • HY-17504D
    (3S,5R)-Rosuvastatin
    		Activator
    (3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    (3S,5R)-Rosuvastatin
  • HY-13629S1
    Etoposide-13C,d3
    		Inducer
    Etoposide-13C,d3 is the 13C- and deuterium labeled Etoposide. Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide-<sup>13</sup>C,d<sub>3</sub>
  • HY-10224S1
    Panobinostat-d4 hydrochloride
    		Inducer
    Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
    Panobinostat-d<sub>4</sub> hydrochloride
  • HY-162084
    BKN-1
    		Inducer
    BKN-1 is a bifunctional ligand that can not only track the formation of mtG4s (G-quadruplexes, four-stranded DNA structures containing Hoogsteen bonds) through far-red emission, but can also induce mitochondrial dysfunction. BKN-1 has anti-tumor activity and may cause mtDNA loss, damage mitochondrial integrity, reduce ATP levels, and trigger ROS imbalance, leading to apoptosis and autophagy.
    BKN-1
  • HY-10539
    Enzastaurin dihydrochloride
    		Inducer
    Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
    Enzastaurin dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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