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-112618A
    Thalidomide-O-amido-C6-NH2 TFA
    		Inducer 99.82%
    Thalidomide-O-amido-C6-NH2 TFA (Cereblon Ligand-Linker Conjugates 11 TFA), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
    Thalidomide-O-amido-C6-NH2 TFA
  • HY-130948B
    Thalidomide-4-O-C4-NH2 hydrochloride
    		Inducer 99.35%
    Thalidomide-4-O-C4-NH2 hydrochloride 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-4-O-C4-NH2 hydrochloride
  • HY-16569S
    Colchicine-d6
    		Inducer 99.41%
    Colchicine-d6 is the deuterium labeled Colchicine. Colchicine is a tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs).
    Colchicine-d<sub>6</sub>
  • HY-17514S1
    Itraconazole-d3
    		99.62%
    Itraconazole-d3 (R51211-d3) is the deuterium labeled Itraconazole (HY-17514). Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects. Itraconazole is a oxysterol-binding protein (OSBP) inhibitor.
    Itraconazole-d<sub>3</sub>
  • HY-114423
    p38α inhibitor 1
    		98.91%
    p38α inhibitor 1 is a p38α inhibitor extracted from patent WO 2008076265 A1.
    p38α inhibitor 1
  • HY-126458
    Thalidomide-O-PEG2-propargyl
    		Inducer 98.26%
    Thalidomide-O-PEG2-propargyl (E3 ligase Ligand-Linker Conjugates 32) is an E3 ligase ligand-linker conjugate. Thalidomide-O-PEG2-propargyl is also a click chemistry reagent containing an alkyne group, which can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAC) with molecules bearing an azide group.
    Thalidomide-O-PEG2-propargyl
  • HY-129703A
    Thalidomide-PEG2-C2-NH2 TFA
    		Inducer 99.13%
    Thalidomide-PEG2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
    Thalidomide-PEG2-C2-NH2 TFA
  • HY-13017S2
    Ivacaftor-d18
    Ivacaftor-d18 is the deuterium labeled Ivacaftor. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
    Ivacaftor-d<sub>18</sub>
  • HY-137978
    Ezurpimtrostat
    		Inhibitor 99.37%
    Ezurpimtrostat (GNS561) is an orally active PPT1 inhibitor, autophagy inhibitor, immunomodulator, anti-inflammatory agent, and anticancer agent. Ezurpimtrostat inhibits PPT1, dysregulates lysosomal function, redistributes mTOR, and induces apoptosis. Ezurpimtrostat reduces IFN‑α, CRP, immune complex deposition, and SARS‑CoV‑2 viral load. Ezurpimtrostat can be used for the study of systemic lupus erythematosus, SARS‑CoV‑2, hepatocellular carcinoma, fibrosis, and related disorders.
    Ezurpimtrostat
  • HY-15206S
    Glyburide-d11
    		Inducer 99.39%
    Glyburide-d11 is the deuterium labeled Glibenclamide. Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
    Glyburide-d<sub>11</sub>
  • HY-131159
    Thalidomide-O-C8-Boc
    		Inducer
    Thalidomide-O-C8-Boc is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-Boc can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-C8-Boc
  • HY-P3491
    Pegloxenatide
    		Modulator
    Pegloxenatide (Polyethylene glycol loxenatide) is a long-acting glucagon-like peptide-1 receptor (GLP-1RA) agonist. Pegloxenatide has various activities such as lowering blood glucose, lowering blood lipids, improving body weight, anti-inflammation, promoting wound healing, protecting the liver, and protecting the heart. Pegloxenatide can be used in the research of type 2 diabetes and its multiple complications.
    Pegloxenatide
  • HY-138773
    Thalidomide-PEG5-COOH
    		Inducer 99.49%
    Thalidomide-PEG5-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-PEG5-COOH
  • HY-138774
    Thalidomide-PEG4-COOH
    		Inducer
    Thalidomide-PEG4-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-PEG4-COOH
  • HY-B1417S
    Nortriptyline-d3 hydrochloride
    		Inducer 99.69%
    Nortriptyline-d3 (hydrochloride) is the deuterium labeled Nortriptyline hydrochloride. Nortriptyline hydrochloride (Desmethylamitriptyline hydrochloride) is a tricyclic antidepressant and the main active metabolite of Amitriptyline, and used to relieve the symptoms of depression.
    Nortriptyline-d<sub>3</sub> hydrochloride
  • HY-N0384S
    Homovanillic acid-d3
    		98.44%
    Homovanillic acid-d3 (Vanilacetic acid-d3) is the deuterium labeled Homovanillic acid (HY-N0384). Homovanillic acid (Vanilacetic acid) is a dopamine metabolite found to be associated with aromatic L-amino acid decarboxylase deficiency, celiac disease, growth hormone deficiency, and sepiapterin reductase deficiency.
    Homovanillic acid-d<sub>3</sub>
  • HY-110231
    Simvastatin-d6
    		Inducer 99.6%
    Simvastatin-d6 (MK 733-d6) is the deuterium labeled Simvastatin. Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
    Simvastatin-d<sub>6</sub>
  • HY-N0480S
    Reserpine-d9
    		Inhibitor
    Reserpine-d9 is the deuterium labeled Reserpine. Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
    Reserpine-d<sub>9</sub>
  • HY-B0965AS
    Thioridazine-d3 hydrochloride
    		Inducer 98.25%
    Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine-d<sub>3</sub> hydrochloride
  • HY-N0824R
    Syringin (Standard)
    		Inhibitor
    Syringin (Standard) is the analytical standard of Syringin. This product is intended for research and analytical applications. Syringin (Eleutheroside B) is an active natural phenolic glycoside possessing various pharmacological activities, including anti-inflammatory, anti-irradiation, anti-osteoporosis and anticancer activities. Syringin also can be used to enhance memory, relieve fatigue, improve human cognition and protect ischemia heart against cerebrovascular damage, etc.
    Syringin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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