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-161197
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
    		Inducer
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
  • HY-116071
    Autophagy-IN-3
    		Inhibitor
    Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments.
    Autophagy-IN-3
  • HY-12515AS2
    Nicardipine-d4 hydrochloride
    		Inducer
    Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
    Nicardipine-d<sub>4</sub> hydrochloride
  • HY-B1039C
    Ambroxol acefylline
    		Inducer
    Ambroxol (NA-872) acefylline, an active metabolite of the proagent Bromhexine, has potent expectorant effects. Ambroxol acefylline is a glucocerebrosidase (GCase) chaperone and increases glucocerebrosidase activity. Ambroxol acefylline induces lung autophagy and has the potential for Parkinson disease and neuronopathic Gaucher disease research.
    Ambroxol acefylline
  • HY-Y0148R
    10-Hydroxydecanoic acid (Standard)
    10-Hydroxydecanoic acid (Standard) is the analytical standard of 10-Hydroxydecanoic acid. This product is intended for research and analytical applications. 10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells[1][2][3][4][5].
    10-Hydroxydecanoic acid (Standard)
  • HY-138850A
    Thalidomide-NH-amido-C3-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-amido-C3-NH2 hydrochloride 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-C3-NH2 hydrochloride
  • HY-W751650
    Sildenafil-d3 citrate
    Sildenafil-d3 citrate (UK-92480-d3 citrate) is the deuterium labeled Sildenafil citrate (HY-15025A). Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil-d<sub>3</sub> citrate
  • HY-170877
    SHP2-IN-35
    		Inducer
    SHP2-IN-35 (Compound 3f) is the inhibitor for SHP2. SHP2-IN-35 exhibits antiproliferative activity in cancer cells RKO, SW480 and CT26 with IC50 of 5.72 μM, 3.71 μM and 1.42 μM, respectively. SHP2-IN-35 inhibits the PI3K-Akt signaling pathway, regulates the cell cycle associated gene expressions, and induces mitochondrial-related autophagy. SHP2-IN-35 inhibits the expression of certain cytokines and chemokines in the tumor microenvironment (TME), thereby regulating the tumor progression.
    SHP2-IN-35
  • HY-158060
    MC2646
    		Inducer
    MC2646 is a potent anti-parasite agent. MC2646 induces autophagic. MC2646 activates the AMPK/TFEB pathway.
    MC2646
  • HY-170670
    DQ661
    		Inhibitor
    DQ661 is a potent PPT1 inhibitor. DQ661 is a dimeric quinacrine autophagy inhibitor. DQ661 inhibits mTORC1 activity. DQ661 decreases the protein expression of pS6K T389, pS6 S240-244. DQ661 shows anticancer activity.
    DQ661
  • HY-N0372R
    Licochalcone A (Standard)
    		Inducer
    Licochalcone A (Standard) is the analytical standard of Licochalcone A. This product is intended for research and analytical applications. Licochalcone A (LCA), a flavonoid isolated, presents obvious anti-cancer effects, displays broad-spectrum inhibition against UDP-glucuronosyltransferases (UGTs). Licochalcone A (LCA) exhibits strong inhibitory effects against UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9, and 2B7 (both IC50 and Ki values lower than 5 μM) .
    Licochalcone A (Standard)
  • HY-13511AS
    Rupatadine-d4 fumarate
    		Inducer
    Rupatadine-d4 fumarate is a deuterium labeled Rupatadine fumarate. Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki values of 0.55/0.1 μM (rabbit platelet membranes/guinea pig cerebellum membranes).
    Rupatadine-d<sub>4</sub> fumarate
  • HY-17473R
    Embelin (Standard)
    		Inducer
    Embelin (Standard) is the analytical standard of Embelin. This product is intended for research and analytical applications. Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
    Embelin (Standard)
  • HY-N2959R
    Brevilin A (Standard)
    		Inducer
    Brevilin A (Standard) is the analytical standard of Brevilin A. This product is intended for research and analytical applications. Brevilin A is an orally active STAT3/JAK inhibitor (STAT3 IC50= 10.6 μM). Brevilin A shows anti-tumor activity, anti-proliferative activity to cancer cells, and can induce apoptosis and autophagy.
    Brevilin A (Standard)
  • HY-N1988R
    Cucurbitacin IIa (Standard)
    		Inducer
    Cucurbitacin IIa (Hemslecin A) (Standard) is the analytical standard for Cucurbitacin IIa (HY-N1988). This product is used for research and analytical applications. Cucurbitacin IIa is an orally active, blood-brain barrier-penetrating EGFR inhibitor with an IC50 of 1.455 nM for human EGFR. Cucurbitacin IIa induces caspase-3 dependent cell apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton through actin aggregation, blocks the cell cycle at the G2/M phase, and inhibits the EGFR-MAPK signaling pathway to exert anti-inflammatory activity. Cucurbitacin IIa can be used in research on inflammatory-related diseases, depression, and non-small cell lung cancer and other cancers.
    Cucurbitacin IIa (Standard)
  • HY-N0103R
    Sophocarpine (Standard)
    		Inducer
    Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
    Sophocarpine (Standard)
  • HY-15449R
    Kaempferide (Standard)
    		Inducer
    Kaempferide (Standard) is the analytical standard of Kaempferide. This product is intended for research and analytical applications.
    Kaempferide (Standard)
  • HY-B0233S1
    Isradipine-d6
    Isradipine-d6 is the deuterium labeled Isradipine. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
    Isradipine-d<sub>6</sub>
  • HY-B0444A
    Maprotiline
    		Inducer
    Maprotiline is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.
    Maprotiline
  • HY-B0193AR
    Prazosin hydrochloride (Standard)
    		Inducer
    Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.
    Prazosin hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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