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-N0191R
    Andrographolide (Standard)
    		Inducer
    Andrographolide (Standard) is the analytical standard of Andrographolide. This product is intended for research and analytical applications. Andrographolide is a NF-κB inhibitor, which inhibits NF-κB activation through covalent modification of a cysteine residue on p50 in endothelial cells without affecting IκBα degradation or p50/p65 nuclear translocation. Andrographolide has antiviral effects.
    Andrographolide (Standard)
  • HY-B0444R
    Maprotiline (hydrochloride) (Standard)
    		Inducer
    Maprotiline (hydrochloride) (Standard) is the analytical standard of Maprotiline (hydrochloride). Maprotiline (hydrochloride) (Standard) is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline (hydrochloride) (Standard) induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.
    Maprotiline (hydrochloride) (Standard)
  • HY-N9341
    Norswertianin
    		Inducer 99.58%
    Norswertianin, a xanthone compound, serves as a powerful anti-glioma compound. Norswertianin induces GBM cells differentiation through oxidative stress and Akt/mTOR dependent autophagy.
    Norswertianin
  • HY-B0968S
    Trimetazidine-d8 dihydrochloride
    		Inducer 99.87%
    Trimetazidine-d8 (dihydrochloride) is the 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[1][2][3][4].
    Trimetazidine-d<sub>8</sub> dihydrochloride
  • HY-B0144AS1
    Pitavastatin-d5 sodium
    		99.53%
    Pitavastatin-d5 (sodium) is the deuterium labeled Pitavastatin sodium. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.
    Pitavastatin-d<sub>5</sub> sodium
  • HY-75124
    (Rac)-AZD 6482
    		Activator 98.51%
    (Rac)-AZD 6482 ((Rac)-KIN-193) is the racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
    (Rac)-AZD 6482
  • HY-14658S
    Thalidomide-d4
    		Inducer 98.00%
    Thalidomide-d4 is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].
    Thalidomide-d<sub>4</sub>
  • HY-B1039AS
    Ambroxol-d5 hydrochloride
    		Inducer 99.46%
    Ambroxol-d5 (hydrochloride) is the deuterium labeled Ambroxol hydrochloride. Ambroxol hydrochloride (NA-872 hydrochloride), an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol hydrochloride is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol hydrochloride induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research[1][2].
    Ambroxol-d<sub>5</sub> hydrochloride
  • HY-14397S
    Indomethacin-d4
    		Inhibitor 99.78%
    Indomethacin-d4 is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells[1]. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes[2].
    Indomethacin-d<sub>4</sub>
  • HY-B0418AS
    Loperamide-d6 hydrochloride
    		Inducer 99.07%
    Loperamide-d6 (hydrochloride) is a deuterium labeled Loperamide hydrochloride. Loperamide hydrochloride is an opioid receptor agonist for the treatment of diarrhea[1].
    Loperamide-d<sub>6</sub> hydrochloride
  • HY-P0271
    Syntide 2
    Syntide 2, a Ca2+- and calmodulin (CaM)-dependent protein kinase II (CaMKII) substrate peptide, selectively inhibits the gibberellin (GA) response, leaving constitutive and abscisic acid-regulated events unaffected.
    Syntide 2
  • HY-B0151S
    Pregnenolone-d4
    		Inducer
    Pregnenolone-d4 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication[1][2]. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels[3].
    Pregnenolone-d<sub>4</sub>
  • HY-44063
    Thalidomide-NH-PEG3-NH-Boc
    		Inducer
    Thalidomide-NH-PEG3-NH-Boc is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-NH-PEG3-NH-Boc acts as a ligand for Cereblon to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-PEG3-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-PEG3-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-NH-PEG3-NH-Boc
  • HY-N2478
    Taraxasteryl acetate
    		Inducer 98.74%
    Taraxasteryl acetate is isolated from P. sagittalis,and has a broad spectrum of anti-inflammatory activity. Taraxasterol acetate promotes RNF31 degradation by activating autophagy. Taraxasteryl acetate relieves dextran, zymosan and arachidonic acid induced rat hind-paw edema. Taraxasteryl acetate can be used for the topical inflammation treatment[1][2].
    Taraxasteryl acetate
  • HY-B0863S
    Glyphosate-d2
    		Inducer 99.73%
    Glyphosate-d2 is the deuterium labeled Glyphosate. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants[1].
    Glyphosate-d<sub>2</sub>
  • HY-N0225R
    (-)-Epigallocatechin (Standard)
    		Inducer
    (-)-Epigallocatechin (Standard) is the analytical standard of (-)-Epigallocatechin. This product is intended for research and analytical applications. (-)-Epigallocatechin (Epigallocatechin) is the most abundant flavonoid in green tea, can bind to unfolded native polypeptides and prevent conversion to amyloid fibrils.
    (-)-Epigallocatechin (Standard)
  • HY-10331S
    Regorafenib-d3
    		Inducer ≥98.0%
    Regorafenib-d3 is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
    Regorafenib-d<sub>3</sub>
  • HY-12163S
    Entinostat-d4
    Entinostat-d4 is the deuterium labeled Entinostat[1]. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively[2].
    Entinostat-d<sub>4</sub>
  • HY-17376R
    Ezetimibe (Standard)
    		Inducer 99.90%
    Ezetimibe (Standard) is the analytical standard of Ezetimibe. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N2113
    Glaucocalyxin B
    		Inducer 99.65%
    Glaucocalyxin B is an ent kaurane diterpenoid isolated from the Chinese traditional medicine Rabdosia japonica with anticancer and antitumor activity; decreases the growth of HL-60 cells with an IC50 of approximately 5.86 μM at 24 h.
    Glaucocalyxin B
Cat. No. Product Name / Synonyms Application Reactivity
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