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-B0492S
    rel-Paroxetine-d4-1 hydrochloride
    (rac)-(trans)-Paroxetine-d4 (hydrochloride) is the deuterium labeled (rac)-(trans)-Paroxetine hydrochloride.
    rel-Paroxetine-d<sub>4</sub>-1 hydrochloride
  • HY-15463S3
    Imatinib-13C,d3
    		Inducer
    Imatinib-13C,d3 (STI571-13C,d3) is 13C labeled Imatinib. Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-10453R
    Ixazomib (Standard)
    		Inducer
    Ixazomib (Standard) is the analytical standard of Ixazomib. This product is intended for research and analytical applications. 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 (Standard)
  • HY-108232R
    MK-2206 (Standard)
    		Inducer
    MK-2206 (Standard) is the analytical standard of MK-2206 (HY-108232). This product is intended for research and analytical applications. MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities.
    MK-2206 (Standard)
  • HY-14151R
    Prucalopride (Standard)
    		Inducer
    Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
    Prucalopride (Standard)
  • HY-131717A
    Thalidomide-NH-CH2-COOH TFA
    		Inducer
    Thalidomide-NH-CH2-COOH TFA is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH TFA can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).
    Thalidomide-NH-CH2-COOH TFA
  • HY-100273R
    AGN 194078 (Standard)
    AGN 194078 (Standard) is the analytical standard of AGN 194078 (HY-100273). This product is intended for research and analytical applications. AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
    AGN 194078 (Standard)
  • HY-160475
    AD-9308
    		Inhibitor
    AD-9308 is a highly selective and orally active ALDH2 activator. AD-9308 activates ALDH2 to promote the clearance of 4-HNE, inhibiting myocardial fibrosis, inflammation and cell apoptosis. AD-9308 improves mitochondrial function, sarcoplasmic reticulum/ endoplasmic reticulum calcium transport and regulates autophagy, restoring intracellular homeostasis. AD-9308 improves the diastolic and systolic function of the heart in diabetic mice and reverses ventricular mal-reconstruction. AD-9308 can be used for the study of diabetic cardiomyopathy.
    AD-9308
  • HY-A0061R
    Trifluridine (Standard)
    		Inducer
    Trifluridine (Standard) is the analytical standard of Trifluridine. This product is intended for research and analytical applications. Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors.
    Trifluridine (Standard)
  • HY-13500R
    GSK343 (Standard)
    		Inducer
    GSK343 (Standard) is the analytical standard of GSK343. This product is intended for research and analytical applications. GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343 (Standard)
  • HY-10405S
    Pamapimod-d4
    Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
    Pamapimod-d<sub>4</sub>
  • HY-103704R
    LY2562175 (Standard)
    LY2562175 (Standard) is the analytical standard of LY2562175 (HY-103704). This product is intended for research and analytical applications. LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
    LY2562175 (Standard)
  • HY-17504BR
    Rosuvastatin Sodium (Standard)
    		Inducer
    Rosuvastatin (Sodium) (Standard) is the analytical standard of Rosuvastatin (Sodium). This product is intended for research and analytical applications. Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin Sodium (Standard)
  • HY-W777418
    Isosorbide mononitrate-13C6
    		Inhibitor
    Isosorbide mononitrate-13C6 (Isosorbide-5-mononitrate-13C6) is 13C-labeled Isosorbide mononitrate (HY-B0642).
    Isosorbide mononitrate-<sup>13</sup>C<sub>6</sub>
  • HY-182824
    Sucrose dilaurate
    		Inducer
    Sucrose dilaurate acts as an emulsifier, dispersant and stabilizer. Sucrose dilaurate reduces the release of HMGB1 from UVB-irradiated keratinocytes. Sucrose dilaurate inhibits melanogenesis and decreases bilirubin levels. Sucrose dilaurate induces autophagy in human epidermal keratinocytes, thereby reducing carboxymethyl lysine (CML) levels. Sucrose dilaurate reduces the secretion of insulin-like growth factor-binding protein 3 (IGFBP3) and nerve growth factor (NGF) by senescent keratinocytes. Sucrose dilaurate is investigated as an emulsifier, dispersant or stabilizer in the cosmetics, food and pharmaceutical industries.
    Sucrose dilaurate
  • HY-A0077R
    Perphenazine (Standard)
    		Inhibitor
    Perphenazine (Standard) is the analytical standard of Perphenazine. This product is intended for research and analytical applications. Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
    Perphenazine (Standard)
  • HY-15136R
    Lonafarnib (Standard)
    		Inducer
    Lonafarnib (Standard) is the analytical standard of Lonafarnib. This product is intended for research and analytical applications. Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities.
    Lonafarnib (Standard)
  • HY-132489S
    (Rac)-Sitagliptin-d4
    		Inhibitor
    (Rac)-Sitagliptin-d4 ((Rac)-MK-0431-d4) is the deuterium labeled (Rac)-Sitagliptin. (Rac)-Sitagliptin is an isoform of Sitagliptin (HY-13749), which is a potent and orally active inhibitor of DPP4 with an IC50 of 19 nM in Caco-2 cell extracts.
    (Rac)-Sitagliptin-d<sub>4</sub>
  • HY-13511R
    Rupatadine (Standard)
    		Inducer
    Rupatadine (Standard) is the analytical standard of Rupatadine. This product is intended for research and analytical applications. Rupatadine (UR-12592) is a potent, orally active and long-lasting dual PAF/H1 antagonist, with Kis of 0.55 μM and 0.1 μM, respectively. Rupatadine can be used for the research of allergic rhinitis and urticaria.
    Rupatadine (Standard)
  • HY-B0338R
    Rimantadine (Standard)
    		Inducer
    Rimantadine (Standard) is the analytical standard of Rimantadine. This product is intended for research and analytical applications. Rimantadine is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity.
    Rimantadine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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