1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

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-10201AR
    Sorafenib tosylate (Standard)
    Inducer
    Sorafenib tosylate (Standard) is the analytical standard of Sorafenib tosylate. This product is intended for research and analytical applications. Sorafenib tosylate (Bay 43-9006 tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib tosylate is a ferroptosis activator.
    Sorafenib tosylate (Standard)
  • HY-50878S1
    Crizotinib-d8
    Inducer
    Crizotinib-d8 (PF-02341066-d8) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib-d<sub>8</sub>
  • HY-16508S1
    Ulipristal acetate-d3
    Inducer
    Ulipristal acetate-d3 (CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
    Ulipristal acetate-d<sub>3</sub>
  • HY-10562R
    Ketanserin (Standard)
    Inducer
    Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
    Ketanserin (Standard)
  • HY-B0803R
    Lumefantrine (Standard)
    Inhibitor
    Lumefantrine (Standard) is the analytical standard of Lumefantrine. This product is intended for research and analytical applications. Lumefantrine is an active antimalarial molecule used in combination with Artemether as a first- and second-line antimalarial drug.
    Lumefantrine (Standard)
  • HY-W653875
    Azithromycin-d5
    Inhibitor
    Azithromycin-d5 (CP-62993-d5) is the deuterium labeled Azithromycin (CP-62993) (HY-17506). Azithromycin is a macrolide antibiotic useful for thestudy of a number of bacterial infections.
    Azithromycin-d<sub>5</sub>
  • HY-W748328
    Ixazomib-13C2,15N
    Inducer
    Ixazomib-13C2,15N is 13C and 15N labeled Ixazomib. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
    Ixazomib-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-B0824A
    (1R)-cis-Bifenthrin
    (1R)-cis-Bifenthrin is a widely used pyrethroid pesticide with activity that reduces motor coordination. (1R)-cis-Bifenthrin has a significant impact on the motor function of ParKin-/- mice, as shown by increased pole climbing time and wheel running Time decreases. Exposure of (1R)-cis-Bifenthrin resulted in a significant reduction in tyrosine hydroxylase-positive cell counts and protein expression. (1R)-cis-Bifenthrin caused increased expression of mitophagy-related proteins LC3B and p62. (1R)-cis-Bifenthrin has a lower binding energy with transferrin and transferrin receptor 2, showing stronger interactions. The biological effects of (1R)-cis-Bifenthrin show relationships with mitophagy and ferroptosis-related pathways.
    (1R)-cis-Bifenthrin
  • HY-B0284S2
    Nifedipine-13C8
    Inducer
    Nifedipine-13C8 is a deuterated labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
    Nifedipine-<sup>13</sup>C<sub>8</sub>
  • HY-12012R
    SB 216763 (Standard)
    Inducer
    SB 216763 (Standard) is the analytical standard of SB 216763. This product is intended for research and analytical applications. SB 216763 is potent, selective and ATP-competitive GSK-3 inhibitor with IC50s of 34.3 nM for both GSK-3α and GSK-3β.
    SB 216763 (Standard)
  • HY-14605R
    Rasagiline mesylate (Standard)
    Inducer
    Rasagiline (mesylate) (Standard) is the analytical standard of Rasagiline (mesylate). This product is intended for research and analytical applications. Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively. Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Rasagiline mesylate (Standard)
  • HY-12452R
    DPN (Standard)
    Inhibitor
    DPN (Standard) is the analytical standard of DPN. This product is intended for research and analytical applications. DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
    DPN (Standard)
  • HY-110093
    UNC0638 hydrate
    Inhibitor
    UNC0638 hydrate selectively inhibits G9a and GLP histone methyltransferases with IC50 of 15 nM and 19 nM, respectively. UNC0638 hydrate inhibits TNBC cell invasion and migration in vitro. UNC0638 hydrate is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 hydrate has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.
    UNC0638 hydrate
  • HY-W739944
    Ambroxol-d5
    Inducer
    Ambroxol-d5 (NA-872-d5) is deuterium labeled Ambroxol. Ambroxol (NA-872), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
    Ambroxol-d<sub>5</sub>
  • HY-14832S1
    Ataluren-13C6
    Ataluren-13C6 (PTC124-13C6) is 13C labeled Ataluren. Ataluren (PTC124) is an orally available CFTR-G542X nonsense allele inhibitor.
    Ataluren-<sup>13</sup>C<sub>6</sub>
  • HY-12053AR
    Vinorelbine ditartrate (Standard)
    Inducer
    Vinorelbine (ditartrate) (Standard) is the analytical standard of Vinorelbine (ditartrate). This product is intended for research and analytical applications. Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM.
    Vinorelbine ditartrate (Standard)
  • HY-B1490AS3
    Imipramine-d4-1
    Inducer
    Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.
    Imipramine-d<sub>4</sub>-1
  • HY-B0968S1
    Trimetazidine-d9 dihydrochloride
    Inducer
    Trimetazidine-d9 (dihydrochloride) is deuterium labeled Trimetazidine (dihydrochloride). Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
    Trimetazidine-d<sub>9</sub> dihydrochloride
  • HY-50673A
    Dactolisib hydrochloride
    Inducer
    Dactolisib (BEZ235) hydrochloride is an orally active, dual pan-class I PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR with IC50 of 4 nM/5 nM/7 nM/75 nM and 20.7 nM, respectively. Dactolisib hydrochloride (BEZ235) inhibits mTORC1 and mTORC2.
    Dactolisib hydrochloride
  • HY-B0265R
    Nimodipine (Standard)
    Inducer
    Nimodipine (Standard) is the analytical standard of Nimodipine. This product is intended for research and analytical applications. Nimodipine (BAY-e 9736) is an orally active, well-tolerated and light-sensitive dihydropyridine calcium antagonist. Nimodipine can be used for the research of cerebrovascular disorders.
    Nimodipine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity