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-10440
    Vismodegib
    		Inducer 99.97%
    Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively.
    Vismodegib
  • HY-15108
    Purmorphamine
    		Inhibitor 99.9%
    Purmorphamine is a smoothened/Smo receptor agonist with an EC50 of 1 μM.
    Purmorphamine
  • HY-112654
    GCN2iB
    		99.83%
    GCN2iB is an ATP-competitive inhibitor of a serine/threonine-protein kinase general control nonderepressible 2 (GCN2), with an IC50 of 2.4 nM.
    GCN2iB
  • 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-12678
    Entrectinib
    		Inducer 99.79%
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib
  • HY-13777
    Zoledronic Acid
    		Inducer 99.00%
    Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
    Zoledronic Acid
  • HY-13324
    Bardoxolone methyl
    		Inducer 99.31%
    Bardoxolone methyl (NSC 713200; RTA 402; CDDO Methyl ester) is a synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities, acting as an activator of the Nrf2 pathway and an inhibitor of the NF-κB pathway.
    Bardoxolone methyl
  • HY-15310
    Ivermectin
    		Inducer 98.28%
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
    Ivermectin
  • HY-13026
    Idelalisib
    		Inducer 99.78%
    Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
    Idelalisib
  • HY-B0260
    Methylprednisolone
    		Inhibitor 99.75%
    Methylprednisolone 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-17504
    Rosuvastatin Calcium
    		Inducer 99.77%
    Rosuvastatin Calcium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin Calcium
  • 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
  • HY-B1370
    Hydroxychloroquine sulfate
    		Inhibitor 99.99%
    Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine sulfate is efficiently inhibits SARS-CoV-2 infection in vitro.
    Hydroxychloroquine sulfate
  • HY-50935
    Troglitazone
    		Inducer 99.78%
    Troglitazone is an orally active PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively. Troglitazone has anticancer activity, prevents and inhibits the development of type 2 diabetes.
    Troglitazone
  • HY-10225
    Belinostat
    		Inducer 99.95%
    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
    Belinostat
  • HY-13780
    Vinblastine sulfate
    		Inducer 99.86%
    Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM.
    Vinblastine sulfate
  • HY-14248
    Letrozole
    		Inducer 99.95%
    Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
    Letrozole
  • HY-13500
    GSK343
    		Inducer 99.88%
    GSK343 is a highly potent and selective EZH2 inhibitor with an IC50 of 4 nM.
    GSK343
  • HY-14393
    Emodin
    		Inhibitor 99.25%
    Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
    Emodin
  • HY-50094
    Pictilisib
    		Inducer 99.80%
    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
    Pictilisib
Cat. No. Product Name / Synonyms Application Reactivity
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