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-101920
    Autophinib
    		Inhibitor 99.95%
    Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
    Autophinib
  • HY-B1077
    Penfluridol
    		Inducer 99.93%
    Penfluridol (R-16341) is a potent, long-acting, first-generation, oral diphenylbutylpiperidine antipsychotic agent by targeting D2-like dopamine receptor. Penfluridol effectively inhibits TNFα-induced NF-κB activation and alleviates the severity of arthritis and colitis in vivo. Penfluridol is a Ca2+-calmodulin inhibitor. Penfluridol induces apoptosis and autophagy. Penfluridol is used for chronic schizophrenia, acute psychosis, Tourette syndrome and autoimmune diseases. Penfluridol inhibites the growth of E. faecalis planktonic cells with the MIC of 7.81 µg/ml.
    Penfluridol
  • HY-N0108
    Physcion
    		99.00%
    Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells.
    Physcion
  • HY-15425A
    PF-543 Citrate
    		Inducer 99.47%
    PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy.
    PF-543 Citrate
  • HY-16558
    Butein
    		Inducer 99.64%
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
    Butein
  • HY-10401
    VX-702
    		99.69%
    VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
    VX-702
  • HY-14598
    Diethylstilbestrol
    		Inducer 99.62%
    Diethylstilbestrol is a non-steroidal female hormone that has oral activity and can act on menopausal and postmenopausal disorders. Diethylstilbestrol can induce DNA oxidation and Apoptosis of spermatogonial stem cells. Diethylstilbestrol can induce thymocyte Autophagy Diethylstilbestrol is a 11β-hydroxysteroid dehydrogenase 2 (HSD11B2) inhibitor..
    Diethylstilbestrol
  • HY-32736
    Triptonide
    		Inducer 99.89%
    Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.
    Triptonide
  • HY-N0703
    Schaftoside
    		99.57%
    Schaftoside is a flavonoid found in a variety of Chinese herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission.
    Schaftoside
  • HY-B0271
    Pyrazinamide
    		Inducer 99.97%
    Pyrazinamide (Pyrazinecarboxamide; Pyrazinoic acid amide) is a potent and orally active antitubercular antibiotic. Pyrazinamide is a proagent that is converted to the active form pyrazinoic acid (POA) by PZase/nicotinamidase encoded by the pncA gene in M. tuberculosis.
    Pyrazinamide
  • HY-Y1362
    Ethyl pyruvate
    		Inducer 99.87%
    Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease.
    Ethyl pyruvate
  • HY-N0330
    Momordin Ic
    		Inducer 99.78%
    Momordin Ic is an orally active triterpenoid saponin that can be isolated from Kochia scoparia. It is also a SUMO specific protease 1 (SENP1) inhibitor, SENP1/c-MYC signaling pathway inhibitor, and apoptosis inducer. Momordin Ic induces autophagy and apoptosis in liver cancer cells through the PI3K/Akt and MAPK signaling pathways mediated by reactive oxygen species. Momordin Ic has the ability to control glucose induced blood glucose elevation, inhibit gastric emptying, resist rheumatoid arthritis, reduce CCl4 (HY-Y0298) induced hepatotoxicity and anti-tumor activity.
    Momordin Ic
  • HY-103157
    PD146176
    		Inducer 99.59%
    PD146176 (NSC168807), a 15-Lipoxygenase (15-LO) inhibitor, inhibits rabbit reticulocyte 15-LO (Ki=197 nM, IC50=0.54 μM). PD146176 reverses cognitive impairment, brain amyloidosis, and tau pathology by stimulating autophagy in aged triple transgenic mice.
    PD146176
  • HY-10212
    BIIB021
    		Inducer 99.19%
    BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.
    BIIB021
  • HY-13606
    Dacinostat
    		Inducer 98.45%
    Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
    Dacinostat
  • HY-111621
    DC661
    		Inhibitor 99.53%
    DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor, inhibits autophagy, and acts as an anti-lysosomal agent. Anti-cancer activity.
    DC661
  • HY-B0309
    Felodipine
    		Inducer 99.83%
    Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier.
    Felodipine
  • HY-N0089
    Schisandrin B
    		Inducer 99.94%
    Schisandrin B (γ-Schisandrin) is a biphenylcyclooctadiene derivative isolated from Schisandra chinensis and has been shown to have antioxidant effects on the liver and heart of rodents.
    Schisandrin B
  • HY-B0532A
    Trifluoperazine dihydrochloride
    		Inhibitor 99.98%
    Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride
  • HY-145752
    HaloPROTAC-E
    		Inhibitor 98.76%
    HaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two Halo-tagged endoplasmic reticulum-localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM. HaloPROTAC-E significantly and selectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) labeled with Halo and inhibits autophagy.
    HaloPROTAC-E
Cat. No. Product Name / Synonyms Application Reactivity
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