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-B1232R
    Metyrapone (Standard)
    		Inducer
    Metyrapone (Standard) is the analytical standard of Metyrapone. This product is intended for research and analytical applications. Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression.
    Metyrapone (Standard)
  • HY-N0052AR
    Sanguinarine chloride (Standard)
    		Inducer
    Sanguinarine (chloride) (Standard) is the analytical standard of Sanguinarine (chloride). This product is intended for research and analytical applications. Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.
    Sanguinarine chloride (Standard)
  • HY-10865R
    LY2183240 (Standard)
    LY2183240 (Standard) is the analytical standard of LY2183240 (HY-10865). This product is intended for research and analytical applications. LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KiAA1363, respectively .
    LY2183240 (Standard)
  • HY-N0589R
    Dehydrodiisoeugenol (Standard)
    		Inhibitor
    Dehydrodiisoeugenol (Standard) is the analytical standard of Dehydrodiisoeugenol (HY-N0589). This product is intended for research and analytical applications. Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol (Standard)
  • HY-B0217R
    Nitazoxanide (Standard)
    		Inducer
    Nitazoxanide (Standard) is the analytical standard of Nitazoxanide. This product is intended for research and analytical applications. Nitazoxanide (NTZ), an anthelmintic agent, exhibits a broad spectrum of activities against a wide variety of helminths, protozoa, and enteric bacteria infecting animals and humans. Nitazoxanide inhibits Giardia lamblia trophozoite proliferation in axenic culture with an IC50 of 2.4 μM. Nitazoxanide can be used for the research of parasitic gastroenteritis. Nitazoxanide shows anti-Japanese encephalitis virus (JEV) activity in a mouse model.
    Nitazoxanide (Standard)
  • HY-N0221S2
    Daurisoline-d11
    		Inhibitor
    Daurisoline-d11 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer.
    Daurisoline-d<sub>11</sub>
  • HY-10358R
    MK-2206 dihydrochloride (Standard)
    		Inducer
    MK-2206 dihydrochloride (MK-2206 2HCl) (Standard) is the analytical standard of MK-2206 dihydrochloride (HY-10358). This product is intended for research and analytical applications. MK-2206 dihydrochloride is an orally active pan-AKT inhibitor, with IC50 values of 8 nM, 12 nM and 65 nM against AKT1, AKT2 and AKT3, respectively. MK-2206 dihydrochloride inhibits the Akt/mTOR signaling pathway and reduces the levels of downstream GSK3β and Mcl-1 via proteasomal degradation. MK-2206 dihydrochloride induces G1-phase cell cycle arrest, apoptosis, epithelial-mesenchymal transition, fibroblast activation and extracellular matrix deposition. MK-2206 dihydrochloride causes transient hyperglycemia and hyperinsulinemia in animals. MK-2206 dihydrochloride can be used in research related to solid tumors, renal fibrosis and hypercholesterolemia.
    MK-2206 dihydrochloride (Standard)
  • HY-15340R
    LG100268 (Standard)
    LG100268 (Standard) is the analytical standard of LG100268. This product is intended for research and analytical applications. LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
    LG100268 (Standard)
  • 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-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-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-10225R
    Belinostat (Standard)
    		Inducer
    Belinostat (Standard) is the analytical standard of Belinostat (HY-10225). This product is intended for research and analytical applications. Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
    Belinostat (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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