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 (988):

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 potent, reversible proteasome inhibitor with an IC50 of 100 nM. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, is an autophagy activator.
  • HY-12320
    Cycloheximide Inhibitor 99.86%
    Cycloheximide (Naramycin A), an antifungal antibiotic, is an eukaryote protein synthesis inhibitor, with IC50s of 532.5 nM and 2880 nM for protein synthesis and RNA synthesis in vivo, respectively. Cycloheximide suppresses ferroptosis and inhibits autophagy.
  • 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 Activator 99.95%
    LY294002 (NSC 697286; SF 1101) 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. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
  • HY-B1227
    Carprofen 99.76%
    Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
  • HY-122614
    S29434 Activator 99.37%
    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production.
  • HY-17567C
    Heparin sodium salt (MW 15kDa) Inhibitor
    Heparin sodium salt (MW 15kDa) (Sodium heparin (MW 15kDa)) is a polymer of Heparin with the molecular weight of 15kDa. Heparin sodium salt is an anticoagulant which binds reversibly to antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin factor IIa and factor Xa.
  • HY-10162
    Olaparib Activator 99.98%
    Olaparib (AZD2281;KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
  • HY-17394
    Cisplatin Activator >99.0%
    Cisplatin (CDDP) is an antineoplastic chemotherapy drug by cross-linking with DNA and causing DNA damage in cancer cells. Cisplatin activates ferroptosis and induces autophagy.
  • HY-17559
    Actinomycin D Activator 99.58%
    Actinomycin D (Dactinomycin) inhibits DNA repair with an IC50 of 0.42 μM. Actinomycin D is an autophagy activator.
  • HY-15142
    Doxorubicin hydrochloride Activator 99.47%
    Doxorubicin hydrochloride (Hydroxydaunorubicin hydrochloride), a cytotoxic anthracycline antibiotic, is an anti-cancer chemotherapy agent. Doxorubicin hydrochloride inhibits topoisomerase II, thus stopping DNA replication. Doxorubicin hydrochloride reduces basal phosphorylation of AMPK and its downstream target acetyl-CoA carboxylase. Doxorubicin hydrochloride induces apoptosis and autophagy.
  • HY-13316
    Mitomycin C Activator 99.45%
    Mitomycin C (Ametycine) is a DNA cross-linking agent and induces DNA damaging. Mitomycin C is an antitumor drug and antibiotic that shows extraordinary ability to inhibit DNA synthesis. Mitomycin C is an ADC Cytotoxin and induces autophagy.
  • HY-11109
    Resatorvid Inhibitor 99.95%
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. 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. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases.
  • HY-17589
    Chloroquine phosphate Inhibitor 99.94%
    Chloroquine phosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro.
  • 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. Venetoclax induces autophagy.
  • HY-100558
    Bafilomycin A1 Inhibitor 99.43%
    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 and induces apoptosis.
  • HY-13030
    (+)-JQ-1 Activator 99.90%
    (+)-JQ-1 (JQ1) 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-B0015
    Paclitaxel Inhibitor 99.97%
    Paclitaxel (Taxol) is a naturally occurring antineoplastic agent and stabilizes tubulin polymerization. Paclitaxel can cause both mitotic arrest and apoptotic cell death. Tubulin depolymerization inhibitor.
  • HY-10256
    SB 203580 Activator 99.92%
    SB 203580 (RWJ 64809) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. SB 203580 inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. SB 203580 does not disrupt JNK activity and is an autophagy and mitophagy activator.
Isoform Specific Products

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