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-P9904
    Atezolizumab
    		Inducer 98.98%
    Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
    Atezolizumab
  • HY-50876
    (E)-Daporinad
    		Inducer 99.91%
    (E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.
    (E)-Daporinad
  • HY-N0504
    Lovastatin
    		99.89%
    Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Lovastatin
  • 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-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-13683
    Mifepristone
    		Inducer 99.83%
    Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
    Mifepristone
  • HY-14590
    Kaempferol
    		Inducer 99.92%
    Kaempferol (Kempferol), a flavonoid found in many edible plants, inhibits estrogen receptor α expression in breast cancer cells and induces apoptosis in glioblastoma cells and lung cancer cells by activation of MEK-MAPK. Kaempferol can be uesd for the research of breast cancer.
    Kaempferol
  • HY-13067
    Celastrol
    		Inducer 99.90%
    Celastrol (Tripterine;Tripterin) is a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. In addition, Celastrol is also an antibiotic with potent antimicrobial activity against standard and clinical methicillin-resistant Staphylococcus aureus (MRSA) strains, inducing oxidative stress and inhibiting DNA synthesis by binding to P5CDH.
    Celastrol
  • HY-10320
    Doramapimod
    		99.98%
    Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
    Doramapimod
  • HY-10971
    Alisertib
    		Inducer 99.84%
    Alisertib (MLN 8237) is an orally active and selective Aurora A kinase inhibitor (IC50=1.2 nM), which binds to Aurora A kinase resulting in mitotic spindle abnormalities, mitotic accumulation. Alisertib (MLN 8237) induces apoptosis and autophagy through targeting the AKT/mTOR/AMPK/p38 pathway in leukemic cells. Antitumor activity.
    Alisertib
  • HY-15979A
    H-89 dihydrochloride
    		Inducer 99.34%
    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-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-B0313
    Hydroxyurea
    		Inducer 99.34%
    Hydroxyurea is a cell apoptosis inducer that inhibit DNA synthesis through inhibition of ribonucleotide reductase. Hydroxyurea shows anti-orthopoxvirus activity.
    Hydroxyurea
  • HY-12222
    Obeticholic acid
    		≥98.0%
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
    Obeticholic acid
  • HY-50855
    Silmitasertib
    		Inducer 99.94%
    Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
    Silmitasertib
  • HY-50907
    ABT-737
    		Inducer 99.96%
    ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.
    ABT-737
  • HY-13768A
    Topotecan hydrochloride
    		Inducer 99.89%
    Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.
    Topotecan hydrochloride
  • HY-100489
    TBHQ
    		Inducer 99.89%
    TBHQ (tert-Butylhydroquinone) is a widely used Nrf2 activator, protects against Doxorubicin (DOX)-induced cardiotoxicity through activation of Nrf2. TBHQ (tert-Butylhydroquinone) is also an ERK activator; rescues Dehydrocorydaline (DHC)-induced cell proliferation inhibitionin melanoma.
    TBHQ
  • HY-12047
    Ponatinib
    		Inducer 99.43%
    Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2/KDR/Flk-1, FGFR1, and Src, respectively.
    Ponatinib
  • HY-12495
    ISRIB (trans-isomer)
    		98.58%
    ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC50 of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC50=5 nM).
    ISRIB (trans-isomer)
Cat. No. Product Name / Synonyms Application Reactivity
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