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-120325
    DHMPA
    		Inducer
    DHMPA is an effective depletor of norepinephrine content of the heart, brain and spleen in mouse and rat. DHMPA has antihypertensive effects.
    DHMPA
  • HY-B0165AS
    Pravastatin-13C,d3 sodium
    Pravastatin-13C,d3 (sodium) is the 13C- and deuterium labeled Pravastatin (sodium). Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin-<sup>13</sup>C,d<sub>3</sub> sodium
  • HY-161198
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc
    		Inducer
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc
  • HY-17504D
    (3S,5R)-Rosuvastatin
    		Activator
    (3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    (3S,5R)-Rosuvastatin
  • HY-13629S1
    Etoposide-13C,d3
    		Inducer
    Etoposide-13C,d3 is the 13C- and deuterium labeled Etoposide. 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[1].
    Etoposide-<sup>13</sup>C,d<sub>3</sub>
  • HY-10224S1
    Panobinostat-d4 hydrochloride
    		Inducer
    Panobinostat-d4 (hydrochloride) is deuterium labeled Panobinostat. Panobinostat (LBH589; NVP-LBH589) is a potent and orally active non-selective HDAC inhibitor, and has antineoplastic activities[1][2]. Panobinostat induces HIV-1 virus production even at low concentration range 8-31 nM, stimulates HIV-1 expression in latently infected cells[4]. Panobinostat induces cell apoptosis and autophagy. Panobinostat can be used for the study of refractory or relapsed multiple myeloma[3].
    Panobinostat-d<sub>4</sub> hydrochloride
  • HY-162084
    BKN-1
    		Inducer
    BKN-1 is a bifunctional ligand that can not only track the formation of mtG4s (G-quadruplexes, four-stranded DNA structures containing Hoogsteen bonds) through far-red emission, but can also induce mitochondrial dysfunction. BKN-1 has anti-tumor activity and may cause mtDNA loss, damage mitochondrial integrity, reduce ATP levels, and trigger ROS imbalance, leading to apoptosis and autophagy.
    BKN-1
  • HY-10539
    Enzastaurin di(hydrochloride)
    		Inducer
    Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
    Enzastaurin di(hydrochloride)
  • HY-B0113S1
    Omeprazole-d3-1
    		Inducer
    Omeprazole-d3-1 is the deuterium labeled Omeprazole. Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM[1]. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria[2].Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[3].
    Omeprazole-d<sub>3</sub>-1
  • HY-B1071R
    Lasalocid (Standard)
    		Inducer
    Lasalocid (Standard) is the analytical standard of Lasalocid. This product is intended for research and analytical applications. Lasalocid (Lasalocid-A; Ionophore X-537A; Antibiotic X-537A) is an antibacterial and anticoccidial agent used in feed additives.
    Lasalocid (Standard)
  • HY-B0561S2
    Spironolactone-d3-1
    		Inducer
    Spironolactone-d3-1 is deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes[1][2][3].
    Spironolactone-d<sub>3</sub>-1
  • HY-15030AR
    Naproxen (sodium) (Standard)
    		Inducer
    Naproxen (sodium) (Standard) is the analytical standard of Naproxen (sodium). This product is intended for research and analytical applications. Naproxen sodium is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
    Naproxen (sodium) (Standard)
  • HY-N0693R
    Schisandrin A (Standard)
    		Inducer
    Schisandrin A (Standard) is the analytical standard of Schisandrin A. This product is intended for research and analytical applications. Schisandrin A inhibits CYP3A activity with an IC50 of 6.60 μM and Ki of 5.83 μM, respectively.
    Schisandrin A (Standard)
  • HY-13018B
    MRT67307 dihydrochloride
    		Inhibitor
    MRT67307 dihydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 dihydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 dihydrochloride also blocks autophagy in cells.
    MRT67307 dihydrochloride
  • HY-B0642R
    Isosorbide mononitrate (Standard)
    		Inhibitor
    Isosorbide mononitrate (Standard) is the analytical standard of Isosorbide mononitrate. This product is intended for research and analytical applications. Isosorbide mononitrate (Isosorbide-5-mononitrate) is a nitric acid compound used for angina pectoris by dilating blood vessels and lowering blood pressure.
    Isosorbide mononitrate (Standard)
  • HY-P1479
    Calmodulin-Dependent Protein Kinase II (290-309)
    Calmodulin-Dependent Protein Kinase II (290-309) is a potent CaMK antagonist with an IC50 of 52 nM for inhibition of Ca2+/calmodulin-dependent protein kinase II.
    Calmodulin-Dependent Protein Kinase II (290-309)
  • HY-111274
    Indomethacin farnesil
    		Inhibitor
    Indomethacin farnesil is an orally active proagent of Indomethacin. Indomethacin (Indometacin) is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
    Indomethacin farnesil
  • HY-168072
    GP130-IN-1
    GP130-IN-1 (compound 49) is a potent GP130 inhibitor with significant in vitro antitumor activity and higher selectivity than Bazedoxifene (HY-A0031). GP130-IN-1 induces ultrastructural changes in cells, causing cell cycle arrest in the G0/G1 phase in a time-dependent manner and triggering apoptosis and autophagy. GP130-IN-1 can be used in the study of triple-negative breast cancer.
    GP130-IN-1
  • HY-12687R
    Tizoxanide (Standard)
    		Inducer
    Tizoxanide (Standard) is the analytical standard of Tizoxanide. This product is intended for research and analytical applications. Tizoxanide (TIZ) is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide (TIZ) has anti-HIV-1 activities and potent inhibition of both HBV and HCV replication with values EC50 of 0.46μM and 0.15 μM, respectively. Tizoxanide also exerts anti-inflammatory effects by inhibiting the production of pro-inflammatory cytokines and suppressing of the activation of the NF-κB and the MAPK signaling pathways in LPS-treated macrophage cells.
    Tizoxanide (Standard)
  • HY-14654C
    Aspirin calcium
    		Inducer
    Aspirin calcium is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin calcium induces apoptosis. Aspirin calcium inhibits the activation of NF-κB. Aspirin calcium also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis.
    Aspirin calcium
Cat. No. Product Name / Synonyms Application Reactivity
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