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-10514
    BX795
    		Modulator 99.84%
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
    BX795
  • HY-15979A
    H-89 dihydrochloride
    		Inducer 99.97%
    H-89 dihydrochloride is a potent and selective inhibitor of protein kinase A (PKA) with an IC50 of 48 nM and has weak inhibition on PKG, PKC, Casein Kinase.
    H-89 dihydrochloride
  • HY-12000
    AG490
    		Inducer 99.86%
    AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
    AG490
  • 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-10159
    Nilotinib
    		Inducer 99.94%
    Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib
  • 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-N1201
    Apigenin
    		Inducer 99.22%
    Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin
  • 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-17356
    Fenofibrate
    		Inducer 99.97%
    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-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-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-13062
    Daunorubicin hydrochloride
    		Inducer 99.67%
    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-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-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-10422
    AZD-8055
    		Inducer 99.60%
    AZD-8055 is a potent, selective, and orally bioavailable ATP-competitive mTOR kinase inhibitor with an IC50 of 0.8 nM. AZD-8055 inhibits both mTORC1 and mTORC2.
    AZD-8055
  • HY-15465
    KN-93
    		99.42%
    KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
    KN-93
  • HY-50108
    GW 4064
    		99.61%
    GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
    GW 4064
  • HY-B0172
    Lithocholic acid
    		Inducer 99.96%
    Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.
    Lithocholic acid
  • HY-12273
    DMH-1
    		Inhibitor 99.95%
    DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5/47.6 nM for ALK1/ALK2/ALK3/ALK6, respectively.
    DMH-1
  • HY-N0176
    Dihydroartemisinin
    		Inducer 99.03%
    Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin
Cat. No. Product Name / Synonyms Application Reactivity
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