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-W739793
    Pantoprazole-d8 sodium
    Pantoprazole-d8 (BY1023-d8) sodium is a deuterium labeled Pantoprazole (HY-17507). Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
    Pantoprazole-d<sub>8</sub> sodium
  • HY-B0715S3
    Pentoxifylline-d3
    		Inducer
    Pentoxifylline-d3 (BL-191-d3) is deuterium labeled Pentoxifylline. Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
    Pentoxifylline-d<sub>3</sub>
  • HY-17356S2
    Fenofibrate-13C6
    		Inducer
    Fenofibrate-13C6 is a deuterated labeled Fenofibrate. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate-<sup>13</sup>C<sub>6</sub>
  • HY-107811R
    Harmol (Standard)
    		Inducer
    Harmol (Standard) is the analytical standard of Harmol (HY-107811). This product is intended for research and analytical applications. Harmol hydrochloride is an orally active β-carboline alkaloid. Harmol hydrochloride is a TFEB activator and monoamine oxidase inhibitor. Harmol can induce cell mitosis, Autophagy and Apoptosis. Harmol promotes the degradation of α-synuclein by regulating the autophagy-lysosomal pathway. Harmol has anti-tumor, anti-depressant and anti-aging activities. Harmol improves motor impairment in a mouse Parkinson's disease model.
    Harmol (Standard)
  • HY-111772R
    Elexacaftor (Standard)
    Elexacaftor (Standard) is the analytical standard of Elexacaftor. This product is intended for research and analytical applications. Elexacaftor (VX-445, Compound 1) is a modulator of cystic fibrosis transmembrane conductance regulator (CFTR). Elexacaftor (VX-445, Compound 1) facilitates the processing and trafficking of CFTR to increase the amount of CFTR at the cell surface.
    Elexacaftor (Standard)
  • HY-10532R
    SRT 1720 (Standard)
    		Inducer
    SRT 1720 (Standard) is the analytical standard of SRT 1720. This product is intended for research and analytical applications. SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively.
    SRT 1720 (Standard)
  • HY-50898R
    Lapatinib (Standard)
    		Inducer
    Lapatinib (Standard) is the analytical standard of Lapatinib. This product is intended for research and analytical applications. Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib (Standard)
  • HY-157514
    Thalidomide 4'-ether-PEG1-azide
    		Inducer
    Thalidomide 4'-ether-PEG1-azide is the Thalidomide (HY-14658)-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4'-ether-PEG1-azide can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide 4'-ether-PEG1-azide
  • HY-N0876R
    Arenobufagin (Standard)
    		Inducer
    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway.
    Arenobufagin (Standard)
  • HY-13677R
    6-Mercaptopurine (Standard)
    		Inhibitor
    6-Mercaptopurine (Standard) is the analytical standard of 6-Mercaptopurine. This product is intended for research and analytical applications. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
    6-Mercaptopurine (Standard)
  • HY-15486R
    Salubrinal (Standard)
    		Inhibitor
    Salubrinal (Standard) is the analytical standard of Salubrinal. This product is intended for research and analytical applications. Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
    Salubrinal (Standard)
  • HY-12542AR
    Dantrolene sodium hemiheptahydrate (Standard)
    		Inhibitor
    Dantrolene (sodium hemiheptahydrate) (Standard) is the analytical standard of Dantrolene (sodium hemiheptahydrate). This product is intended for research and analytical applications. Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
    Dantrolene sodium hemiheptahydrate (Standard)
  • HY-160896
    Autophagy-IN-5
    		Inhibitor
    Autophagy-IN-5 (Compound A9) is an inhibitor for autophagy with an EC50 of 0.736 μM.
    Autophagy-IN-5
  • HY-N0163R
    Magnolol (Standard)
    		Inducer
    Magnolol (Standard) is the analytical standard of Magnolol. This product is intended for research and analytical applications. Magnolol, a natural lignan isolated from the stem bark of Magnolia officinalis, is a dual agonist of both RXRα and PPARγ, with EC50 values of 10.4 μM and 17.7 μM, respectively.
    Magnolol (Standard)
  • HY-50898CS
    Lapatinib-d4 tosylate
    		Inducer
    Lapatinib-d4 (GW572016-d4) tosylate is deuterium labeled Lapatinib (tosylate). Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib-d<sub>4</sub> tosylate
  • HY-131611R
    6-Azuridine (Standard)
    		Activator
    6-Azuridine (Standard) is the analytical standard of 6-Azuridine. This product is intended for research and analytical applications. 6-Azuridine (6-Azauridine) is an orally active purine nucleoside analogue. 6-Azuridine activates autophagic flux, induces Apoptosis that depends on AMPK and p53. 6-Azuridine exhibit both antitumor and antiviral activities.
    6-Azuridine (Standard)
  • HY-N1508R
    Ecliptasaponin A (Standard)
    		Inducer
    Ecliptasaponin A (Standard) is the analytical standard for Ecliptasaponin A (HY-N1508). Ecliptasaponin A is an orally active pentacyclic triterpenoid saponin. Ecliptasaponin A exerts anti-tumor activity by activating ASK1/JNK pathway, inducing apoptosis and autophagy in lung cancer cells. Ecliptasaponin A exerts anti-inflammatory/anti-fibrotic effects and protects the cardiovascular system by inhibiting the HMGB1/TLR4/NF-κB pathway, and the expression of COX-2 and MMP-9. Ecliptasaponin A can enhance SOD activity, reduce MDA levels, and alleviate oxidative stress damage. Ecliptasaponin A exerts chondroprotective effects by inhibiting the expression of MMP13 and regulating inflammatory factors. Ecliptasaponin A improves ovarian function and regulates sex hormones by upregulating the expression of ESR1 receptors.
    Ecliptasaponin A (Standard)
  • HY-W018791R
    Bifendate (Standard)
    		Inhibitor
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).
    Bifendate (Standard)
  • HY-N0221S
    Daurisoline-d2
    		Inhibitor
    Daurisoline-d2 is the deuterium labeled Daurisoline (HY-N0221). Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer.
    Daurisoline-d<sub>2</sub>
  • HY-12273G
    DMH-1 (GMP)
    		Inducer
    DMH-1 (GMP) is a GMP-grade version of DMH-1 (HY-12273). Small molecules of GMP grade can be used as adjuvant reagents in cell therapy. DMH-1 (GMP) promotes cardiac differentiation in mouse embryonic stem cells. DMH-1 (GMP) promotes neurogenesis of hiPSCs. DMH-1 is a potent and selective BMP inhibitor.
    DMH-1 (GMP)
Cat. No. Product Name / Synonyms Application Reactivity
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