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-10261
    Afatinib
    		Inducer 99.92%
    Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib
  • HY-12248
    Telaglenastat
    		Inducer 99.82%
    Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity.
    Telaglenastat
  • HY-10455
    Carfilzomib
    		Inducer 99.98%
    Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of 5 nM in ANBL-6 and RPMI 8226 cells.
    Carfilzomib
  • HY-10331
    Regorafenib
    		Inducer 99.93%
    Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/Flt-1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity.
    Regorafenib
  • HY-16569
    Colchicine
    		Inducer 99.95%
    Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.
    Colchicine
  • HY-15304
    Dynasore
    		Inducer 99.66%
    Dynasore is a cell-permeable dynamin inhibitor with an IC50 of 15 μM. Dynasore blocks cell migration.
    Dynasore
  • HY-12057
    Vemurafenib
    		Inducer 99.85%
    Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
    Vemurafenib
  • HY-101840
    EIPA
    		Activator 99.73%
    EIPA (L593754) is an orally active TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also enhances autophagy by inhibiting Na+/H+-exchanger 3 (NHE3). EIPA inhibits macropinocytosis as well. EIPA can be used in the research of inflammation and cancers, such as gastric cancer, colon carcinoma, pancreatic carcinoma.
    EIPA
  • HY-15463
    Imatinib
    		Inducer 99.95%
    Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
    Imatinib
  • HY-10231
    PX-478
    		Inhibitor ≥98.0%
    PX-478 is an orally active HIF-1α inhibitor with potent antitumor activities. PX-478 can cross the blood-brain barrier.
    PX-478
  • HY-10255A
    Sunitinib
    		Inducer 99.04%
    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2/KDR/Flk-1 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
    Sunitinib
  • HY-13823
    C646
    		Inducer 99.88%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
    C646
  • HY-B0589
    Atorvastatin
    		Inducer 99.82%
    Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin
  • HY-10029
    Nutlin-3a
    		Inducer 99.00%
    Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53?interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53?wild-type ovarian carcinomas.
    Nutlin-3a
  • 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-P9904
    Atezolizumab
    		Inducer 99.50%
    Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
    Atezolizumab
  • HY-12163
    Entinostat
    		Inducer 99.82%
    Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
    Entinostat
  • HY-17471A
    Metformin hydrochloride
    		Inducer 99.98%
    Metformin (1,1-Dimethylbiguanide) hydrochloride inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin hydrochloride also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, metformin hydrochloride regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
    Metformin hydrochloride
  • 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-B0351
    Taurine
    		Inducer 99.88%
    Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
    Taurine
Cat. No. Product Name / Synonyms Application Reactivity
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