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-130948
    Thalidomide-O-C4-NH2
    		Inducer
    Thalidomide-O-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C4-NH2
  • HY-B0084S1
    Dienogest-d5
    		Inducer
    Dienogest-d5 is deuterium labeled Dienogest.
    Dienogest-d<sub>5</sub>
  • HY-162311
    Anticancer agent 194
    		Inducer
    Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can't induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS.
    Anticancer agent 194
  • HY-10820BR
    Pemetrexed (disodium heptahydrate) (Standard)
    		Inducer
    Pemetrexed (disodium heptahydrate) (Standard) is the analytical standard of Pemetrexed (disodium heptahydrate). This product is intended for research and analytical applications. Pemetrexed disodium heptahydrate is a novel antifolate, the Ki values of the pentaglutamate of LY231514 are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed (disodium heptahydrate) (Standard)
  • HY-161209
    Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-boc
    		Inducer
    Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-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-2,6-diazaspiro[3.4]octane-C-Pip-boc
  • HY-N0176S3
    Dihydroartemisinin-d5
    		Inducer
    Dihydroartemisinin-d5 is deuterated labeled Dihydroartemisinin (HY-N0176). Dihydroartemisinin is a potent anti-malaria agent.
    Dihydroartemisinin-d<sub>5</sub>
  • HY-10999S1
    Trametinib-13C6
    		Inducer
    Trametinib-13C6 is the 13C-labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis[1][2].
    Trametinib-<sup>13</sup>C<sub>6</sub>
  • HY-163230
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc
    		Inducer
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc
  • HY-N0504S2
    Lovastatin-d3
    Lovastatin-d3 is deuterium labeled Lovastatin. Lovastatin is a cell-permeable HMG-CoA reductase inhibitor used to lower cholesterol.
    Lovastatin-d<sub>3</sub>
  • HY-161183
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc
    		Inducer
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-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.
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc
  • HY-B0271S1
    Pyrazinamide-13C,15N
    		Inducer
    Pyrazinamide-13C,15N is 15N and 13C labeled Pyrazinamide (HY-B0271). 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-<sup>13</sup>C,<sup>15</sup>N
  • HY-77591S
    Cysteamine-d4 hydrochloride
    		Modulator
    Cysteamine-d4 (hydrochloride) is the deuterium labeled Cysteamine hydrochloride. Cysteamine hydrochloride (2-Aminoethanethiol hydrochloride) is an orally active agent for the treatment of nephropathic cystinosis and an antioxidant.
    Cysteamine-d<sub>4</sub> hydrochloride
  • HY-W013780S
    Fmoc-Pro-OH-1-13C
    		Inducer
    Fmoc-Pro-OH-1-13C is a 13C-labeled Sulfabenzamide. Sulfabenzamide (N-Sulfanilylbenzamide) is an antimicrobial agent and usually consumed in combination with Sulfathiazole and Sulfacetamide. Sulfabenzamide is effective against Gram-positive and negative ba
    Fmoc-Pro-OH-1-<sup>13</sup>C
  • HY-B0228S2
    Adenosine-2′-13C
    Adenosine-2′-13C is the 13C labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiolo
    Adenosine-2′-<sup>13</sup>C
  • HY-113909
    Dinoprost (methoxyamine)
    		Inducer
    Dinoprost methoxyamine is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost methoxyamine is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost methoxyamine plays a key role in the onset and progression of labour.
    Dinoprost (methoxyamine)
  • HY-124761
    Poloppin
    		Inhibitor
    Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors.
    Poloppin
  • HY-111287
    Autophagonizer
    		Inducer
    Autophagonizer (DK-1-49) is a small molecule autophagy inducer that results in an accumulation of autophagy-associated LC3-II and enhances levels of autophagosomes and acidic vacuoles. Autophagonizer inhibits cell viability and induces cell death in not only cancer cells but also Bax/Bak double-knockout cells with EC50 values of 3-4 μM.
    Autophagonizer
  • HY-162344
    Ir-CA
    		Inducer
    Ir-CA is an antitumor agent. Ir-CA can accumulate in mitochondria and induces mitochondria dysfunction. Ir-CA induces apoptosis and autophagy. Ir-CA initiates mitophagy and cell cycle arrest to kill Cisplatin (HY-17394)-resistant A549R cells. Ir-CA can effectively inhibit metastasis by inhibiting MMP-2/MMP-9.
    Ir-CA
  • HY-163136A
    Autophagy/REV-ERB-IN-1 hydrochloride
    		Inhibitor
    Autophagy/REV-ERB-IN-1 hydrochloride (Compound 24) is a dual autophagy and REV-ERB inhibitor with anticancer activity. Autophagy/REV-ERB-IN-1 (hydrochloride) has improved potency in blocking autophagy, enhanced toxicity against cancer cells. Autophagy/REV-ERB-IN-1 (hydrochloride) can be used for the research for melanoma.
    Autophagy/REV-ERB-IN-1 hydrochloride
  • HY-B1227S
    Carprofen-d3
    Carprofen-d3 is the deuterium labeled Carprofen. Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
    Carprofen-d<sub>3</sub>
Cat. No. Product Name / Synonyms Application Reactivity
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