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-100263B
    Metofenazate diethanesulfonate
    Metofenazate diethanesulfonate is a selective calmodulin inhibitor.
    Metofenazate diethanesulfonate
  • HY-13748R
    Silybin A (Standard)
    		Inducer
    Silybin A (Standard) is the analytical standard of Silybin A. This product is intended for research and analytical applications. Silybin A (Silibinin A), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
    Silybin A (Standard)
  • HY-101744
    Ipsalazide
    Ipsalazide is a novel sulfasalazine analog designed to release 5-aminosalicylic acid and a nontoxic carrier molecule in the gastrointestinal tract.
    Ipsalazide
  • HY-N0370R
    Bergapten (Standard)
    		Inducer
    Bergapten (Standard) is the analytical standard of Bergapten. This product is intended for research and analytical applications. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten (Standard)
  • HY-183660
    F-SLOH
    		Inducer
    F-SLOH is a brain-penerant and orally active TFEB activator and amyloid-β inhibitor with an IC50 of 3.4 μM against amyloid-β. F-SLOH promotes nuclear translocation of TFEB, driving autophagy and lysosomal biogenesis. F-SLOH reduces amyloid-β oligomers and Tau aggregates via autophagy lysosomal degradation pathway. F-SLOH can be used for the research of Alzheimer’s disease.
    F-SLOH
  • HY-17000R
    Tolvaptan (Standard)
    		Inducer
    Tolvaptan (Standard) is the analytical standard of Tolvaptan. This product is intended for research and analytical applications. Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V2R) antagonist with an IC50 of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia.
    Tolvaptan (Standard)
  • HY-N0221R
    Daurisoline (Standard)
    		Inhibitor
    Daurisoline (Standard) is the analytical standard of Daurisoline. This product is intended for research and analytical applications. 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 (Standard)
  • HY-164479
    GA001
    		Inducer
    GA001 is a potent G9a antagonist, with an IC50 of 1.32 μM. GA001 induces autophagy and apoptosis that can be used for the breast cancer.
    GA001
  • HY-14376R
    Redafamdastat (Standard)
    Redafamdastat (Standard) is the analytical standard of Redafamdastat. This product is intended for research and analytical applications. Redafamdastat (PF-04457845) is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.
    Redafamdastat (Standard)
  • HY-15202S1
    Binimetinib-d3
    		Inhibitor
    Binimetinib-d3 (MEK162-d3) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib-d<sub>3</sub>
  • HY-10295AR
    SB 202190 hydrochloride (Standard)
    		Inducer
    SB 202190 (hydrochloride) (Standard) is the analytical standard of SB 202190 (hydrochloride). This product is intended for research and analytical applications. SB 202190 hydrochloride is a selective p38 MAP kinase inhibitor with IC50s of 50 nM and 100 nM for p38α and p38β2, respectively. SB 202190 hydrochloride binds to the ATP pocket of the active recombinant human p38 kinase with a Kd of 38 nM. SB 202190 hydrochloride has anti-cancer activity. SB202190 hydrochloride induces autophagy.
    SB 202190 hydrochloride (Standard)
  • HY-10510R
    BI-D1870 (Standard)
    		Inducer
    BI-D1870 (Standard) is the analytical standard of BI-D1870 (HY-10510). This product is intended for research and analytical applications. BI-D1870 is an ATP-competitive, cell permeable and brain penetrated inhibitor of RSK isoforms, with IC50s of 31 nM/24 nM/18 nM/15 nM for RSK1/RSK2/RSK3/RSK4, respectively.
    BI-D1870 (Standard)
  • HY-B1125S
    Glucosamine-13C6
    		Inducer
    Glucosamine-13C6 (D-Glucosamine-13C6) is 13C labeled Glucosamine. Glucosamine (D-Glucosamine) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine-<sup>13</sup>C<sub>6</sub>
  • HY-N0716
    Berberine
    		Modulator
    Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Berberine (Natural Yellow 18) has antineoplastic properties. The sulfate form (HY-N0716B) improves bioavailability.
    Berberine
  • HY-14171R
    Bexarotene (Standard)
    		Inducer
    Bexarotene (Standard) is the analytical standard of Bexarotene. This product is intended for research and analytical applications. Bexarotene (LGD1069) is a high-affinity and selective retinoid X receptors (RXR) agonist with EC50s of 33, 24, 25 nM for RXRα, RXRβ, and RXRγ, respectively. Bexarotene shows limited affinity for RAR receptors (EC50 >10000 nM). Bexarotene can be used for the research of cutaneous T-cell lymphoma.
    Bexarotene (Standard)
  • HY-17000S
    Tolvaptan-d7
    		Inducer
    Tolvaptan-d7 is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM for the inhibition of AVP-induced platelet aggregation.
    Tolvaptan-d<sub>7</sub>
  • HY-N6687R
    Calcimycin (Standard)
    		Modulator
    Calcimycin (Standard) is the analytical standard of Calcimycin. This product is used for research and analytical applications. Calcimycin is an antibiotic and a unique divalent cation ionophore, such as calcium ions and magnesium ions. Calcimycin induces Ca2+ -dependent cell death by increasing the intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi, and also inhibits the activity of ATPase and uncouples the oxidative phosphorylation (OXPHOS) of mammalian cells, inducing apoptosis and autophagy.
    Calcimycin (Standard)
  • HY-50896S2
    Erlotinib-d4
    		Inducer
    Erlotinib-d4 (CP-358774-d4) is deuterium labeled Erlotinib. Erlotinib (CP-358774) is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer. Erlotinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-d<sub>4</sub>
  • HY-B0180S2
    Imiquimod-d7
    		Inducer
    Imiquimod-d7 (R 837-d7) is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod-d<sub>7</sub>
  • HY-B0113S4
    Omeprazole-d3 sodium
    Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). Omeprazole sodium (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole sodium competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole sodium inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole sodium inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole sodium alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole sodium aslo has neuroprotective and antibacterial effects.
    Omeprazole-d<sub>3</sub> sodium
Cat. No. Product Name / Synonyms Application Reactivity
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