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-75839R
    Dronedarone Hydrochloride (Standard)
    		Inducer
    Dronedarone (Hydrochloride) (Standard) is the analytical standard of Dronedarone (Hydrochloride). This product is intended for research and analytical applications. Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
    Dronedarone Hydrochloride (Standard)
  • HY-W744243
    Etoposide-d4
    Etoposide-d4 (VP-16-d4; VP-16-213-d4) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16; VP-16-213) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide-d<sub>4</sub>
  • HY-B0151S3
    Pregnenolone-d6
    Pregnenolone-d6 (3β-Hydroxy-5-pregnen-20-one-d6) is the deuterium labeled Pregnenolone (HY-B0151) . Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
    Pregnenolone-d<sub>6</sub>
  • HY-169155
    OsMo
    		Modulator
    OsMo is a lysosome-targeting hNEU1 inhibitor that can be used in the study of myocardial injury.
    OsMo
  • HY-13065R
    Isobavachalcone (Standard)
    		Inducer
    Isobavachalcone (Standard) is the analytical standard of Isobavachalcone. This product is intended for research and analytical applications. Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). Isobavachalcone also induces Reactive Oxyen Species (ROS) generation in OVCAR-8 cells and has exhibit cancer anti-promotive and anti-proliferative activity.
    Isobavachalcone (Standard)
  • HY-B0116S
    Stavudine-d4
    		Inducer
    Stavudine-d4 is the deuterium labeled Stavudine. Stavudine (d4T) is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Stavudine has activity against HIV-1 and HIV-2. Stavudine also inhibits the replication of mitochondrial DNA (mtDNA). Stavudine reduces NLRP3 inflammasome activation and modulates Amyloid-β autophagy. Stavudine induces apoptosis.
    Stavudine-d<sub>4</sub>
  • HY-18629A
    (E/Z)-SU9516
    		Inducer
    (E/Z)-SU9516 is the isomer of SU9516 (HY-18629). SU9516 is a potent CDK2 inhibitor，with an IC50 of 22 nM，and also shows inhibitory effects on CDK1 and CDK4，with IC50s of 40，200 nM，respectively.
    (E/Z)-SU9516
  • HY-174292
    YTK-1305
    		Activator
    YTK-1305 is a p62 ligand compound that promotes cellular autophagy.
    YTK-1305
  • HY-P0175A
    740 Y-P TFA
    		Inducer
    740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
    740 Y-P TFA
  • HY-B2031S1
    Pyriproxyfen-d4
    Pyriproxyfen-d4 (S-31183-d4) is the deuterium labeled Pyriproxyfen. Pyriproxyfen is a juvenile hormone analog and insect growth regulator. Pyriproxyfen is used in research related to dengue fever and malaria.
    Pyriproxyfen-d<sub>4</sub>
  • HY-183838
    Autophagy-IN-11
    		Inhibitor
    Autophagy-IN-11 is an ATG5-targeting autophage inhibitor. Autophagy-IN-11 disrupts protein-protein interactions between ATG5 and ATG16L1, and between ATG5 and TECAIR. Autophagy-IN-11 can be used for cancer research.
    Autophagy-IN-11
  • HY-181850
    Telomeric G4s ligand 2
    		Inducer
    Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC50 of 0.4 μM. Telomeric G4s ligand 2 binds to dimeric telomeric G4, inhibits the activities of DHX36 and BLM helicases. Telomeric G4s ligand 2 activates cGAS-STING and TERRA-ZBP1 pathways, inducing autophagy and G2/M cell cycle arrest, and exhibits antiproliferative effects across cancer cell lines. Telomeric G4s ligand 2 can be used for the study of colorectal cancer.
    Telomeric G4s ligand 2
  • HY-138852
    Thalidomide-NH-amido-C6-NH2
    		Inducer
    Thalidomide-NH-amido-C6-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C6-NH2
  • HY-149565
    Thalidomide-5-O-C8-NH2 hydrochloride
    		Inducer
    Thalidomide-5-O-C8-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C8-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C8-NH2 hydrochloride
  • HY-12176S2
    Aliskiren-d6-1 hemifumarate
    		Inducer
    Aliskiren-d6-1 hemifumarate (CGP 60536-d6-1 hemifumarate) is the deuterium labeled Aliskiren hemifumarate (HY-12177). Aliskiren is an orally active, highly potent and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.
    Aliskiren-d<sub>6</sub>-1 hemifumarate
  • HY-10261AR
    Afatinib dimaleate (Standard)
    		Inducer
    Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate). This product is intended for research and analytical applications. Afatinib (BIBW 2992) dimaleate 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 dimaleate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.
    Afatinib dimaleate (Standard)
  • HY-139545
    Thalidomide-4-C3-NH2 hydrochloride
    		Inducer
    Thalidomide-4-C3-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-C3-NH2 hydrochloride
  • HY-149560
    Thalidomide-5-O-C3-NH2 hydrochloride
    		Inducer 99.08%
    Thalidomide-5-O-C3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C3-NH2 hydrochloride
  • HY-10291R
    Tarenflurbil (Standard)
    Tarenflurbil (Standard) is the analytical standard of Tarenflurbil. This product is intended for research and analytical applications. Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.
    Tarenflurbil (Standard)
  • HY-183829
    ATG5-TECAIR-IN-2
    		Inducer
    ATG5-TECAIR-IN-2 is a ATG5 inhibitor with autophagy inhibitory activity. ATG5-TECAIR-IN-2 selectively inhibits the ATG5-TECAIR interaction (IC50=31.24 μM) and shows no activity against the ATG5-ATG16L1 interaction.
    ATG5-TECAIR-IN-2
Cat. No. Product Name / Synonyms Application Reactivity
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