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-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-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-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-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-17504AS1
    Rosuvastatin-d6
    		Inducer
    Rosuvastatin-d6 (ZD 4522-d6) is deuterium labeled Rosuvastatin. Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks hERG current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin-d<sub>6</sub>
  • HY-B0294R
    Flubendazole (Standard)
    		Inducer
    Flubendazole (Standard) is the analytical standard of Flubendazole. This product is intended for research and analytical applications. Flubendazole is an anthelmintic drug based on altering microtubule structure, inhibition of tubulin polymerization and disruption of microtubule function. Flubendazole induces apoptosis in human colorectal cancer (CRC) by blocking the STAT3 signaling axis and activation of autophagy. Flubendazole induces P53 expression and reduced Cyclin B1 and p-cdc2 expression. Flubendazole is an antitumor agent. Flubendazole can be used for worm and intestinal parasites.
    Flubendazole (Standard)
  • HY-A0077S2
    Perphenazine-d6 fumarate
    		Inhibitor
    Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine. Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
    Perphenazine-d<sub>6</sub> fumarate
  • 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-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[1][2].
    Tolvaptan-d<sub>7</sub>
  • HY-N6687R
    Calcimycin (Standard)
    		Modulator
    N-Desalkylflurazepam (Standard) is the analytical standard of N-Desalkylflurazepam. This product is intended for research and analytical applications. N-Desalkylflurazepam (Norfludiazepam) is a long-acting metabolite of benzodiazepine compounds, such as Flurazepam. N-Desalkylflurazepam inhibits L-type voltage-gated calcium channels with IC50 values of 55 μM and 37 μM for Cav1.2 and Cav1.3, respectively.
    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
    		Inducer
    Omeprazole-d3 sodium is deuterated labeled Omeprazole (HY-B0113). 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. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
    Omeprazole-d<sub>3</sub> sodium
  • HY-17364R
    Temozolomide (Standard)
    		Inducer
    Temozolomide (Standard) is the analytical standard of Temozolomide. This product is intended for research and analytical applications. Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
    Temozolomide (Standard)
  • HY-134314
    8-Nitro-cGMP
    		Inducer
    8-Nitro-cGMP is an electrophilic second messenger of redox signaling that can form a protein-S-cGMP adduct in s-guanylation process. 8-Nitro-cGMP is an autophagy inducer. 8-Nitro-cGMP promotes RANKL-induced osteoclast differentiation from macrophages. 8-Nitro-cGMP has vasodilator effect, and ameliorates the vascular endothelial dysfunction in diabetic mice.
    8-Nitro-cGMP
Cat. No. Product Name / Synonyms Application Reactivity
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