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-70002S
    Deutenzalutamide-d3
    		Inducer 99.80%
    Deutenzalutamide (Enzalutamide-d3) is a developed deuterium labeled Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
    Deutenzalutamide-d<sub>3</sub>
  • HY-B0309S2
    Felodipine-d3
    		Inducer 99.78%
    Felodipine-d3 is the deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
    Felodipine-d<sub>3</sub>
  • HY-B0809S
    Theophylline-d6
    		Inhibitor 99.30%
    Theophylline-d6 is the deuterium labeled Theophylline. Theophylline is a nonselective phosphodiesterase (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.
    Theophylline-d<sub>6</sub>
  • HY-B1203AR
    Fludrocortisone acetate (Standard)
    		Inducer
    Fludrocortisone acetate (Standard) is the analytical standard of Fludrocortisone acetate. This product is intended for research and analytical applications.
    Fludrocortisone acetate (Standard)
  • HY-148556
    Thalidomide-O-C6-azide
    		Inducer 99.10%
    Thalidomide-O-C6-azide is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C6-azide is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Thalidomide-O-C6-azide
  • HY-17356S
    Fenofibrate-d6
    		Inducer 99.70%
    Fenofibrate-d6 is the deuterium labeled Fenofibrate. 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-d<sub>6</sub>
  • HY-150407
    TSPO ligand-1
    		Inducer 98.0%
    TSPO ligand-1 is the ligand of AUTAC4 (HY-134640) that can be used in the synthesis of PROTACs. TSPO ligand-1 is a mitochondrial outer membrane transmembrane structural domain protein can bind to AUTAC4 and regulate mitochondrial autophagy to promote targeted mitochondrial renewal. TSPO ligand-1 is also involved in the transport of cholesterol from the outer to inner mitochondrial membrane and serves as a sensitive biomarker of brain injury and neurodegeneration.
    TSPO ligand-1
  • HY-171047
    Autophagy inducer 7
    		Inducer 99.45%
    Autophagy inducer 7 (Compound SSA) is an Autophagy and Apoptosis inducer. Autophagy inducer 7 activates autophagy by inhibiting Akt/mTOR signaling and the expression of downstream proteins. Autophagy inducer 7 suppresses DNA synthesis and causes a G0-G1 cell-cycle arrest. Autophagy inducer 7 inhibits tumor cell growth.
    Autophagy inducer 7
  • HY-161872
    LC3in-C42
    		Inhibitor
    LC3in-C42 is a cell-active LC3A/B and autophagy covalent inhibitor. LC3in-C42 selectively inhibits the binding of P62 to LC3A/B in vitro and at the cellular level like D5 and can function on a lower concentration.
    LC3in-C42
  • HY-N0136A
    (±)-Taxifolin
    		Inhibitor 99.34%
    (±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin (HY-N0136). Taxifolin 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
  • HY-133780
    Afatinib impurity 11
    		Inducer 99.10%
    Afatinib impurity 11 is an impurity of Afatinib. Afatinib is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
    Afatinib impurity 11
  • HY-N0305S1
    5-Aminolevulinic acid-d2 hydrochloride
    		Inducer
    5-Aminolevulinic acid-d2 (hydrochloride) is deuterium labeled 5-Aminolevulinic acid (hydrochloride).
    5-Aminolevulinic acid-d<sub>2</sub> hydrochloride
  • HY-15448S
    Tezacaftor-d4
    		Inducer 98.95%
    Tezacaftor-d4 (VX-661-d4) is the deuterium-labeled Tezacaftor (HY-15448), a F508del CFTR corrector. Tezacaftor helps CFTR protein reach the cell surface.
    Tezacaftor-d<sub>4</sub>
  • HY-103691A
    ARN5187 trihydrochloride
    		Inhibitor 99.54%
    ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis.
    ARN5187 trihydrochloride
  • HY-N9942
    Physalin A
    		Inducer 99.63%
    Physalin A is a biologically active withanolide. Physalin A shows anti-inflammatory, antifibrotic and ameliorative effects on autophagy in models of disc degeneration. Physalin A has antitumor activity and can induce apoptosis, ROS production and G2/M phase cell cycle arrest. Besides. Physalin A can significantly increase the activity of quinone reductase and increase the expression of detoxifying enzymesc.
    Physalin A
  • 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-N0076R
    Bilobalide (Standard)
    		Inhibitor
    Bilobalide (Standard) is the analytical standard of Bilobalide. This product is intended for research and analytical applications. Bilobalide, a sesquiterpene trilactone constituent of Ginkgo biloba, inhibits the NMDA-induced efflux of choline with an IC50 value of 2.3 μM. Bilobalide prevents apoptosis through activation of the PI3K/Akt pathway in SH-SY5Y cells. Exerts protective and trophic effects on neurons.
    Bilobalide (Standard)
  • HY-10181R
    Dasatinib (Standard)
    		Inducer
    Dasatinib (Standard) is the analytical standard of Dasatinib. This product is intended for research and analytical applications. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib (Standard)
  • HY-10219S1
    Rapamycin-13C,d3
    		Inducer
    Rapamycin-13C,d3 (Sirolimus-13C,d3) is the 13C and deuterium labeled Rapamycin (HY-10219). Rapamycin is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
    Rapamycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-100973AR
    Adenosine 5′-diphosphoribose sodium (Standard)
    		Inducer
    Adenosine 5′-diphosphoribose (sodium) (Standard) is the analytical standard of Adenosine 5′-diphosphoribose (sodium). This product is intended for research and analytical applications. Adenosine 5′-diphosphoribose sodium (ADP ribose sodium) is a nicotinamide adenine nucleotide (NAD+) metabolite. Adenosine 5′-diphosphoribose sodium is the most potent and primary intracellular Ca2+-permeable cation TRPM2 channel activator. Adenosine 5′-diphosphoribose sodium also can enhance autophagy.
    Adenosine 5′-diphosphoribose sodium (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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