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-10194A
    Sepantronium hydrochloride
    		Inducer
    Sepantronium hydrochloride (YM-155 hydrochloride) is a novel survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.
    Sepantronium hydrochloride
  • HY-B1490AR
    Imipramine (Standard)
    		Inducer
    Imipramine (Standard) is the analytical standard of Imipramine. This product is intended for research and analytical applications. 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 (Standard)
  • HY-10404R
    Dilmapimod (Standard)
    Dilmapimod (Standard) is the analytical standard of Dilmapimod. This product is intended for research and analytical applications. Dilmapimod (SB-681323) is a potent p38 MAPK inhibitor that potentially suppresses inflammation in chronic obstructive pulmonary disease.
    Dilmapimod (Standard)
  • HY-100532R
    CD437 (Standard)
    CD437 (Standard) is the analytical standard of CD437. This product is intended for research and analytical applications. CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
    CD437 (Standard)
  • HY-B1693R
    Levomepromazine (Standard)
    		Inducer
    Levomepromazine (Standard) is the analytical standard of Levomepromazine. This product is intended for research and analytical applications. Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
    Levomepromazine (Standard)
  • HY-15247R
    Vistusertib (Standard)
    		Inducer
    Vistusertib (Standard) is the analytical standard of Vistusertib. This product is intended for research and analytical applications. Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes.
    Vistusertib (Standard)
  • HY-15206S2
    Glibenclamide-13C6
    		Inducer
    Glibenclamide-13C6 (Glyburide-13C6) is 13C 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.
    Glibenclamide-<sup>13</sup>C<sub>6</sub>
  • HY-N0504S
    Epi lovastatin-d3
    Epi Lovastatin-d3 is the deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Epi lovastatin-d<sub>3</sub>
  • HY-162100
    MR-2088
    		Inhibitor
    MR-2088 is a selective ULK1/ULK2 inhibitor with pEC50 values of 8.3 and 8.7, respectively. MR-2088 selectively inhibits autophagy through ULK1/2 mediated inhibition.
    MR-2088
  • HY-10158S1
    Bosutinib-13C,d3
    		Inducer
    Bosutinib-13C,d3 (SKI-606-13C,d3) is 13C labeled Bosutinib. Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively.
    Bosutinib-<sup>13</sup>C<sub>,d<sub>3</sub>
  • HY-17401R
    Ranolazine dihydrochloride (Standard)
    		Inducer
    Ranolazine (dihydrochloride) (Standard) is the analytical standard of Ranolazine (dihydrochloride). This product is intended for research and analytical applications. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
    Ranolazine dihydrochloride (Standard)
  • HY-B1077R
    Penfluridol (Standard)
    		Inducer
    Penfluridol (Standard) is the analytical standard of Penfluridol. This product is intended for research and analytical applications. Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml.
    Penfluridol (Standard)
  • HY-13262R
    Lumacaftor (Standard)
    Lumacaftor (Standard) is the analytical standard of Lumacaftor. This product is intended for research and analytical applications. Lumacaftor (VX-809; VRT 826809) is a CFTR modulator that corrects the folding and trafficking of CFTR protein.
    Lumacaftor (Standard)
  • HY-14541A
    Olanzapine hydrochloride
    		Inducer
    Olanzapine hydrochloride is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine hydrochloride is an atypical antipsychotic.
    Olanzapine hydrochloride
  • HY-10181AR
    Dasatinib hydrochloride (Standard)
    		Inducer
    Dasatinib (hydrochloride) (Standard) is the analytical standard of Dasatinib (hydrochloride). This product is intended for research and analytical applications. Dasatinib (BMS-354825) hydrochloride 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 hydrochloride inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib hydrochloride also induces apoptosis and autophagy.
    Dasatinib hydrochloride (Standard)
  • HY-15250R
    JZL195 (Standard)
    JZL195 (Standard) is the analytical standard of JZL195. This product is intended for research and analytical applications. JZL195 is a selective and efficacious dual fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) inhibitor with IC50s of 2 and 4 nM, respectively.
    JZL195 (Standard)
  • HY-14171S2
    Bexarotene-13C6
    		Inducer
    Bexarotene-13C6 (LGD1069-13C6) is 13C labeled Bexarotene. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
    Bexarotene-<sup>13</sup>C<sub>6</sub>
  • HY-10179R
    Danusertib (Standard)
    		Inducer
    Danusertib (Standard) is the analytical standard of Danusertib. This product is intended for research and analytical applications. Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
    Danusertib (Standard)
  • HY-N0487R
    Glucosamine sulfate (Standard)
    		Inducer
    Glucosamine (sulfate) (Standard) is the analytical standard of Glucosamine (sulfate). This product is intended for research and analytical applications. Glucosamine sulfate (D-Glucosamine sulfate) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine sulfate (Standard)
  • HY-12075R
    LY2109761 (Standard)
    		Inhibitor
    LY2109761 (Standard) is the analytical standard of LY2109761. This product is intended for research and analytical applications. LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
    LY2109761 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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