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-10231
    PX-478
    		Inhibitor 99.58%
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
    PX-478
  • HY-13418
    Dorsomorphin dihydrochloride
    		Inhibitor 99.91%
    Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599).
    Dorsomorphin dihydrochloride
  • HY-P0018
    Pepstatin
    		Inhibitor 99.90%
    Pepstatin (Pepstatin A) is a specific, orally active aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin also inhibits HIV protease.
    Pepstatin
  • HY-17362
    Vancomycin hydrochloride
    		Inhibitor 99.47%
    Vancomycin hydrochloride is an antibiotic for the treatment of bacterial infections. It acts by inhibiting the second stage of cell wall synthesis of susceptible bacteria. Vancomycin also alters the permeability of the cell membrane and selectively inhibits ribonucleic acid synthesis.
    Vancomycin hydrochloride
  • HY-44134
    Dimethyl 2-oxoglutarate
    		Inhibitor
    Dimethyl 2-oxoglutarate (Dimethyl α-ketoglutarate) is a cell-permeable derivative of 2-oxoglutarate and tricarboxylic acid cycle metabolite with antioxidant properties. Dimethyl 2-oxoglutarate inhibits Autophagy. Dimethyl 2-oxoglutarate prevents mitochondrial damage and reduces ROS production. Dimethyl 2-oxoglutarate alleviates Carbon tetrachloride (HY-Y0298)-induced liver fibrosis. Dimethyl-2-oxoglutaric acid can be used in the research of diseases such as Alzheimer's disease, diabetes, and cardiomyopathy.
    Dimethyl 2-oxoglutarate
  • HY-18072
    GSK2606414
    		Inhibitor 99.91%
    GSK2606414 is a cell-permeable and orally available protein kinase R-like endoplasmic reticulum (ER) kinase (PERK) inhibitor with an IC50 of 0.4 nM.
    GSK2606414
  • HY-W031727
    Hydroxychloroquine
    		Inhibitor 99.82%
    Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling.
    Hydroxychloroquine
  • HY-B0671
    Vancomycin
    		Inhibitor 99.39%
    Vancomycin is an antibiotic for the treatment of bacterial infections.
    Vancomycin
  • HY-17589
    Chloroquine phosphate
    		Inhibitor 99.89%
    Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine phosphate
  • HY-10211
    Tanespimycin
    		Inhibitor 99.01%
    Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
    Tanespimycin
  • HY-100596
    AS1842856
    		Inhibitor 99.88%
    AS1842856, a specific Foxo1 inhibitor (IC50=30 nM), potently suppresses autophagy. AS1842856 reduces Foxo1 activity and, to a lesser extent, inhibits Foxo1 protein expression by simply binding to Foxo1.
    AS1842856
  • HY-12016
    KU-55933
    		Inhibitor 99.92%
    KU-55933 is a potent ATM inhibitor with an IC50 and Ki of 12.9 and 2.2 nM, respectively, and is highly selective for ATM as compared to DNA-PK, PI3K/PI4K, ATR and mTOR.
    KU-55933
  • HY-10941
    VER-155008
    		Inhibitor 99.82%
    VER-155008 is an inhibitor of Hsp70, with IC50s of 0.5 μM, 2.6 μM, and 2.6 μM for Hsp70, Hsc70 and Grp7, respectively, and with a Kd of 0.3 μM for Hsp70.
    VER-155008
  • HY-15108
    Purmorphamine
    		Inhibitor 99.9%
    Purmorphamine is a smoothened/Smo receptor agonist with an EC50 of 1 μM.
    Purmorphamine
  • HY-100202
    TPEN
    		Inhibitor 99.91%
    TPEN (TPEDA) is a specific cell-permeable heavy metal chelator. TPEN has a higher affinity for Zn2+, but a lower affinity for Mg2+ and Ca2+. TPEN induces DNA damage and increases intracellular ROS production. TPEN also inhibits cell proliferation and induces apoptosis.
    TPEN
  • HY-15282
    E-64
    		Inhibitor 99.96%
    E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC50 of 9 nM for papain.
    E-64
  • HY-16966
    SBI-0206965
    		Inhibitor 99.92%
    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2. SBI-0206965 is also an AMPK inhibitor that can paradoxically increase Thr172 phosphorylation.
    SBI-0206965
  • HY-B0260
    Methylprednisolone
    		Inhibitor 99.78%
    Methylprednisolone (U 7532) is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone
  • HY-113596
    Acetyl Coenzyme A trisodium
    		Inhibitor 99.22%
    Acetyl-coenzyme A (Acetyl-CoA) trisodium is a membrane-impermeant central metabolic intermediate, participates in the TCA cycle and oxidative phosphorylation metabolism. Acetyl-coenzyme A trisodium, regulates various cellular mechanisms by providing (sole donor) acetyl groups to target amino acid residues for post-translational acetylation reactions of proteins. Acetyl Coenzyme A trisodium is also a key precursor of lipid synthesis.
    Acetyl Coenzyme A trisodium
  • HY-Y1269
    Ammonium chloride, AR, 99.5%
    		Inhibitor 99.69%
    Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor. Ammonium chloride is also a lysosome inhibitor.
    Ammonium chloride, AR, 99.5%
Cat. No. Product Name / Synonyms Application Reactivity
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