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-B0098AR
    Doxazosin (mesylate) (Standard)
    		Inducer
    Doxazosin (mesylate) (Standard) is the analytical standard of Doxazosin (mesylate). This product is intended for research and analytical applications. Doxazosin mesylate (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
    Doxazosin (mesylate) (Standard)
  • HY-B0492S
    rel-Paroxetine-d4-1 hydrochloride
    (rac)-(trans)-Paroxetine-d4 (hydrochloride) is the deuterium labeled (rac)-(trans)-Paroxetine hydrochloride[1].
    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-10221R
    Vorinostat (Standard)
    		Inducer
    Vorinostat (Standard) is the analytical standard of Vorinostat. This product is intended for research and analytical applications. Vorinostat (SAHA) is a potent and orally active pan-inhibitor of HDAC1, HDAC2 and HDAC3 (Class I), HDAC6 and HDAC7 (Class II) and HDAC11 (Class IV), with ID50 values of 10 nM and 20 nM for HDAC1 and HDAC3, respectively. Vorinostat induces cell apoptosis. Vorinostat is also an effective inhibitor of human papillomaviruse (HPV)-18 DNA amplification.
    Vorinostat (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-B0309R
    Felodipine (Standard)
    		Inducer
    Felodipine (Standard) is the analytical standard of Felodipine. This product is intended for research and analytical applications. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
    Felodipine (Standard)
  • 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-I0501R
    2'-Aminoacetophenone (Standard)
    2'-Aminoacetophenone (Standard) is the analytical standard of 2'-Aminoacetophenone. This product is intended for research and analytical applications. 2'-Aminoacetophenone is an orally active inducer of apoptosis and respiratory biomarker. 2'-Aminoacetophenone can be used to detect Pseudomonas aeruginosa infections in the lungs of cystic fibrosis patients. 2'-Aminoacetophenone can inhibit the protein levels of LC3BII and p62 in macrophages infected with pqsA or mvfR and regulate autophagy. 2'-Aminoacetophenone can disrupt mitochondrial function by inducing oxidative stress and apoptosis signaling, leading to dysfunction in mouse skeletal muscle.
    2'-Aminoacetophenone (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[1][2].
    Pamapimod-d<sub>4</sub>
  • HY-N0156R
    Oleanolic acid (Standard)
    		Inducer
    Oleanolic acid (Standard) is the analytical standard of Oleanolic acid. This product is intended for research and analytical applications. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities.
    Oleanolic acid (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-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-50895S2
    Gefitinib-d3
    		Inducer
    Gefitinib-d3 (ZD1839-d3) is the deuterium labeled Gefitinib. Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy. Gefitinib has antitumour activity[1][2].
    Gefitinib-d<sub>3</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-168295
    p62-ZZ Ligand-Linker Conjugate 1
    p62-ZZ Ligand-Linker Conjugate 1 is a p62-ZZ domain ligand-linker conjugate. p62-ZZ Ligand-Linker Conjugate 1 can be used to synthesize AUTOTAC VinclozolinM2-2204 (HY-161741).
    p62-ZZ Ligand-Linker Conjugate 1
  • HY-12176R
    Aliskiren (Standard)
    		Inducer
    Aliskiren (Standard) is the analytical standard of Aliskiren. This product is intended for research and analytical applications. Aliskiren is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
    Aliskiren (Standard)
  • HY-10562AR
    Ketanserin tartrate (Standard)
    		Inducer
    Ketanserin (tartrate) (Standard) is the analytical standard of Ketanserin (tartrate). This product is intended for research and analytical applications. Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
    Ketanserin tartrate (Standard)
  • HY-112903A
    YW3-56 hydrochloride
    		Inhibitor
    YW3-56 (hydrochloride) is a PAD inhibitor. YW3-56 (hydrochloride) activates p53 target genes. YW3-56 (hydrochloride) activates ATF and blocks autophagy flux. YW3-56 induces ER stress through the PERK-eIF2α-ATF4 signaling cascade and inhibits the mTOR signaling. YW3-56 (hydrochloride) inhibits triple-negative breast cancer.
    YW3-56 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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