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-B0180
    Imiquimod
    		Inducer 99.96%
    Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod
  • HY-50108
    GW 4064
    		99.61%
    GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
    GW 4064
  • HY-W031727
    Hydroxychloroquine
    		Inhibitor ≥98.0%
    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-13062
    Daunorubicin hydrochloride
    		Inducer 99.62%
    Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin hydrochloride
  • HY-B1081A
    Oxidopamine hydrobromide
    		Inducer 99.95%
    Oxidopamine (6-OHDA) hydrobromide is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrobromide is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrobromide promotes COX-2 activation, leading to PGE2 synthesis and pro-inflammatory cytokine IL-1β secretion. Oxidopamine hydrobromide can be used for the research of Parkinson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.
    Oxidopamine hydrobromide
  • HY-N6687
    Calcimycin
    		Modulator 99.12%
    Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.
    Calcimycin
  • HY-12031A
    U0126
    		Inhibitor 98.45%
    U0126 is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC50s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.
    U0126
  • HY-13814
    PR-619
    		Inducer 99.38%
    PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.
    PR-619
  • HY-B0671
    Vancomycin
    		Inhibitor 99.76%
    Vancomycin is an antibiotic for the treatment of bacterial infections.
    Vancomycin
  • HY-16141
    Cilengitide
    		Inducer 99.80%
    Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers.
    Cilengitide
  • HY-15979
    H-89
    		Inducer 99.54%
    H-89 is a potent and selective inhibitor of cyclic AMP-dependent protein kinase (protein kinase A) with IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase, and others kinases.
    H-89
  • HY-17356
    Fenofibrate
    		Inducer 99.93%
    Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate
  • 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-101491
    SR-18292
    		99.82%
    SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
    SR-18292
  • HY-N1201
    Apigenin
    		Inducer 99.58%
    Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin
  • HY-10941
    VER-155008
    		Inhibitor 99.91%
    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-N0176
    Dihydroartemisinin
    		Inducer 99.03%
    Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin
  • HY-12702
    10058-F4
    		99.77%
    10058-F4 is a c-Myc inhibitor that prevents c-Myc-Max dimerization and transactivation of c-Myc target gene expression.
    10058-F4
  • HY-17538
    ZLN005
    		99.92%
    ZLN005 is a potent activator of peroxisome proliferator-activated receptor-γ coactivator-1α (PGC-1α).
    ZLN005
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
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