1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

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.

Autophagy Related Products (909):

Cat. No. Product Name Effect Purity
  • HY-10219
    Rapamycin Activator 99.93%
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
  • HY-13259
    MG-132 Activator >98.0%
    MG-132 is a peptide aldehyde and a potent, reversible, and cell-permeable proteasome inhibitor with an IC50 of 100 nM, and effectively blocks the proteolytic activity of the 26S proteasome complex.
  • HY-12320
    Cycloheximide Inhibitor 99.86%
    Cycloheximide (Naramycin A) is an eukaryote protein synthesis inhibitor, with IC50s of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively.
  • HY-19312
    3-Methyladenine Inhibitor 99.84%
    3-Methyladenine is a PI3K inhibitor. 3-Methyladenine is a widely used inhibitor of autophagy via its inhibitory effect on class III PI3K.
  • HY-10108
    LY294002 Inhibitor 99.95%
    LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM.
  • HY-100868
    JPH203 Activator 98.67%
    JPH203 is a potent and selective L-type amino acid transporter 1 (LAT-1) inhibitor.
  • HY-115453
    UBCS039 98.55%
    UBCS039 is the first synthetic, specific Sirtuin 6 (SIRT6) activator, inducing autophagy in human tumor cells, with an EC50 of 38 μM.
  • HY-111772
    CFTR corrector 1 99.70%
    CFTR corrector 1 (compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). CFTR corrector 1 (compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
  • HY-10162
    Olaparib Activator 99.98%
    Olaparib (AZD2281;KU0059436) is a potent and oral PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively.
  • HY-17559
    Actinomycin D Activator 99.89%
    Actinomycin D inhibits DNA repair with an IC50 of 0.42 μM.
  • HY-11109
    Resatorvid Inhibitor 99.95%
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases. Resatorvid inhibits NO, TNF-R and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF.
  • HY-15142
    Doxorubicin hydrochloride Activator 99.47%
    Doxorubicin hydrochloride is a cytotoxic anthracycline antibiotic for the treatment of multiple cancers. The possible mechanisms by which doxorubicin acts in the cancer cell are intercalation into DNA and disruption of topoisomerase-II-mediated DNA repair. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase.
  • HY-13030
    (+)-JQ-1 Activator 99.90%
    (+)-JQ-1 is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy.
  • HY-13316
    Mitomycin C Activator 99.45%
    Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis. Mitomycin C is a DNA cross-linking agent, which induces DNA damaging.
  • HY-10256
    SB 203580 Activator 99.92%
    SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor. SB 203580 (RWJ 64809) inhibits SAPK2a/p38 and SAPK2b/p38β2, with IC50s of 50 nM and 500 nM, respectively. LCK, GSK3β and PKBα are also inhibited by SB 203580 (RWJ 64809), but the IC50s are 100-500-fold higher than that for SAPK2a/p38.
  • HY-12041
    SP600125 Inhibitor 98.82%
    SP600125 is a cell-permeable, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively.
  • HY-17589
    Chloroquine diphosphate Inhibitor 99.94%
    Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs).
  • HY-100558
    Bafilomycin A1 Inhibitor >99.0%
    Bafilomycin A1, a macrolide antibiotic isolated from the Streptomyces species, is a specific inhibitor of vacuolar-type H+ ATPase (V-ATPase). Bafilomycin A1 inhibits autophagy.
  • HY-15531
    Venetoclax Activator 99.95%
    Venetoclax (ABT-199; GDC-0199) is a highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM.
  • HY-B0015
    Paclitaxel Inhibitor 99.97%
    Paclitaxel (Taxol), a naturally occurring antineoplastic agent, stabilizes tubulin polymerization, resulting in arrest at the G2/M phase of the cell cycle and apoptotic cell death.
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