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-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-131867
    Thalidomide-NH-PEG1-NH2 hydrochloride
    		Inducer 99.59%
    Thalidomide-NH-PEG1-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-PEG1-NH2 hydrochloride
  • HY-N3225
    Myricanol
    		Inducer 98.93%
    Myricanol is a diarylheptanoid and a Nampt activator. Myricanol exerts anti-inflammatory effects and alleviates glucocorticoid-induced muscle atrophy by increasing Sirtuin 1 (SIRT1) and PRDX5 activities while regulating inflammatory factors. Myricanol exhibits growth inhibition and induces apoptosis in human lung adenocarcinoma A549 cells. Myricanol promotes autophagy-mediated clearance of microtubule-associated protein tau to exert neuroprotective effects. Myricanol protects cardiovascular function by inhibiting PDGFRβ and NF-κB signaling pathways. Myricanol activates mitochondrial transcription factor A (TFAM) expression to exert anti-renal fibrosis effects. Myricanol improves insulin resistance through AMPK activation.
    Myricanol
  • HY-100709
    ZPCK
    		Inducer 99.0%
    ZPCK is an oral active proagent of gemcitabine that was designed for improved oral bioavailability.
    ZPCK
  • HY-114118S1
    Semaglutide-d8 tetraTFA
    		Inducer 99.87%
    Semaglutide-d8 tetraTFA is the deuterium labeled Semaglutide (HY-114118). Semaglutide is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
    Semaglutide-d<sub>8</sub> tetraTFA
  • HY-N1399
    Androsin
    		Inducer 99.94%
    Androsin is an active compound isolated from Picrorhiza Kurroa Royle ex Benth. Androsin activates AMPKα/PI3K/Beclin1/LC3 signaling pathway, inhibits SREBP1c/FASN signaling pathway. Androsin can be used in research of asthma and non-alcoholic fatty liver disease (NAFLD). Androsin is orally active.
    Androsin
  • HY-79511
    FAAH-IN-2
    		99.12%
    FAAH-IN-2 (O-Desmorpholinopropyl Gefitinib) is an inhibitor of FAAH. FAAH-IN-2 is a metabolite of Gefitinib (HY-50895).
    FAAH-IN-2
  • HY-161740
    PHTPP-1304
    		Inducer 99.96%
    PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ.
    PHTPP-1304
  • HY-17376S
    Ezetimibe-d4
    		98.84%
    Ezetimibe-d4 (SCH 58235-d4) is the deuterium labeled Ezetimibe (HY-17376). Ezetimibe (SCH 58235) is a potent cholesterol absorption inhibitor. Ezetimibe is a Niemann-Pick C1-like1 (NPC1L1) inhibitor, and is a potent Nrf2 activator.
    Ezetimibe-d<sub>4</sub>
  • HY-129704B
    Thalidomide-NH-C6-NH2 hydrochloride
    		Inducer 99.62%
    Thalidomide-NH-C6-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-C6-NH2 hydrochloride
  • HY-103611
    Thalidomide-O-amido-PEG3-C2-NH2 TFA
    		Inducer 99.55%
    Thalidomide-O-amido-PEG3-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.
    Thalidomide-O-amido-PEG3-C2-NH2 TFA
  • HY-N0144R
    Piperine (Standard)
    		Inducer
    Piperine (Standard) is the analytical standard of Piperine. This product is intended for research and analytical applications. Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL.
    Piperine (Standard)
  • HY-13538A
    Gemcitabine elaidate hydrochloride
    		Inducer
    Gemcitabine elaidate (CP-4126) hydrochloride is lipophilic pro-agent of Gemcitabine. Gemcitabine elaidate hydrochloride is converted to Gemcitabine by esterases in order to be phosphorylated. Gemcitabine elaidate hydrochloride exhibits anti-tumor activity.
    Gemcitabine elaidate hydrochloride
  • HY-N0462R
    Corilagin (Standard)
    		Inducer
    Corilagin (Standard) is the analytical standard of Corilagin. This product is intended for research and analytical applications. Corilagin, a gallotannin, has anti-tumor, anti-inflammatory and hepatoprotective activities. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin also inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows anti-tumor activity on hepatocellular carcinoma and ovarian cancer model. Corilagin shows low toxicity to normal cells and tissues.
    Corilagin (Standard)
  • HY-W344044
    Levomepromazine maleate
    		Inducer 99.92%
    Levomepromazine maleate (Methotrimeprazine maleate) is an N-substituted phenylthiazine antipsychotic sedative that blocks multiple receptors. Levomepromazine maleate is a potent inhibitor of CYP2D6 and is useful in the study of schizophreni.
    Levomepromazine maleate
  • HY-100779
    Rimacalib
    		99.14%
    Rimacalib (SMP 114) is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
    Rimacalib
  • HY-124729A
    (Rac)-BL-918
    		Inducer 98.88%
    (Rac)-BL-918 is the racemate of BL-918. BL-918 is a potent activator of UNC-51-like kinase 1 (ULK1), inducing cytoprotective autophagy for Parkinson’s disease treatment.
    (Rac)-BL-918
  • HY-17356R
    Fenofibrate (Standard)
    		Inducer
    Fenofibrate (Standard) is the analytical standard of Fenofibrate. This product is intended for research and analytical applications. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate (Standard)
  • HY-13669R
    Lomustine (Standard)
    		Inducer
    Lomustine (Standard) is the analytical standard of Lomustine. This product is intended for research and analytical applications. Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.
    Lomustine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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