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-17026S
    Gemcitabine-13C,15N2
    		Inducer 99.23%
    antimetabolite and an antineoplastic agent. Gemcitabine inhibits DNA synthesis and repair, resulting in autophagyand apoptosis.
    Gemcitabine-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-50751S
    Linifanib-d4
    		Inducer
    Linifanib-d4 (ABT-869-d4; AL-39324-d4) is deuterium-labeled Linifanib (HY-50751).
    Linifanib-d<sub>4</sub>
  • HY-10585AR
    Valproic acid sodium (Standard)
    		Inducer
    Valproic acid (sodium) (Standard) is the analytical standard of Valproic acid (sodium). This product is intended for research and analytical applications. Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid sodium (Standard)
  • HY-17506S1
    Azithromycin-13C,d3
    		99.90%
    Azithromycin-13C,d3 is the deuterium and 13C labeled Azithromycin.
    Azithromycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-B1839R
    Fluazinam (Standard)
    		Activator
    Fluazinam (Standard) is the analytical standard of Fluazinam (HY-B1839). This product is intended for research and analytical applications. Fluazinam is a broad spectrum pyridinamine fungal inhibitor. Fluazinam is an orally active dinitroaniline fungicide. Fluazinam induces phosphorylation of JNK, activates p38 pathway, decreases Bcl-2, activates caspase-3, decreases complex I activity, increases Autophagy and Apoptosis. Fluazinam has strong antifungal activity against F. fujikuroi and B. maydis. Fluazinam has a negative impact on Brachydanio rerio and worker bees.
    Fluazinam (Standard)
  • HY-18672
    SMER18
    		Activator 98.64%
    SMER18 is a small molecule enhancer of rapamycin which act as a mTOR-independent autophagy inducer.
    SMER18
  • HY-B0589E
    Atorvastatin hemicalcium trihydrate
    		Inducer 99.70%
    Atorvastatin hemicalcium trihydrate is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin hemicalcium trihydrate inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.
    Atorvastatin hemicalcium trihydrate
  • HY-B0968S
    Trimetazidine-d8 dihydrochloride
    		Inducer 99.87%
    Trimetazidine-d8 (dihydrochloride) is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
    Trimetazidine-d<sub>8</sub> dihydrochloride
  • HY-14248S
    Letrozole-d4
    		Inducer 99.23%
    Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
    Letrozole-d<sub>4</sub>
  • HY-50895S
    Gefitinib-d8
    		Inducer 98.42%
    Gefitinib-d8 (ZD1839-d8) is a deuterium labeled Gefitinib. Gefitinib is an EGFR tyrosine kinase inhibitor, with IC50 of 2-37 nM in NR6wtEGFR cells.
    Gefitinib-d<sub>8</sub>
  • HY-101923A
    LYN-1604 hydrochloride
    		Activator
    LYN-1604 hydrochloride is a potent UNC-51-like kinase 1 (ULK1) activator (EC50=18.94 nM) for the research of triple negative breast cancer (TNBC).
    LYN-1604 hydrochloride
  • HY-15604A
    AZD1208 hydrochloride
    		Inducer
    AZD1208 hydrochloride is an orally bioavailable, highly selective PIM kinases inhibitor.
    AZD1208 hydrochloride
  • HY-134183
    AUTAC1
    		Inducer
    AUTAC1 is a MetAP2-targeting autophagy-mediated degrader (AUTAC). AUTACs contain a degradation tag and a warhead to provide target specificity. AUTAC1 contains an FBnG (p-Fluorobenzyl Guanine) and a Fumagillol moiety. Fumagillol binds covalently to MetAP2.
    AUTAC1
  • HY-115560A
    Thalidomide-O-amido-C3-NH2 TFA
    		Inducer 99.58%
    Thalidomide-O-amido-C3-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-amido-C3-NH2 TFA
  • HY-B0960S
    Sulfabenzamide-d4
    		99.74%
    Sulfabenzamide (N-Sulfanilylbenzamide)-d4 is the deuterium labeled Sulfabenzamide (HY-B0960). Sulfabenzamide is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
    Sulfabenzamide-d<sub>4</sub>
  • HY-117273
    AZ304
    		Inhibitor 99.77%
    AZ304 is an ATP-competitive dual BRAF kinase inhibitor, potently inhibits wild type BRAF, V600E mutant BRAF and wild type CRAF, with IC50s of 79 nM, 38 nM and 68 nM, respectively. AZ304 also has significant effect on other kinases, such as p38 (IC50, 6 nM), CSF1R (IC50, 35 nM). Anti-tumor activity.
    AZ304
  • HY-14649S3
    Retinoic acid-d6
    		98.9%
    Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
    Retinoic acid-d<sub>6</sub>
  • HY-130854
    Thalidomide-NH-C6-NH-Boc
    		Inducer
    Thalidomide-NH-C6-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used for MI-389 (compound 22) synthesis. MI-389 is a potent phthalimide PROTAC degrader based on the multi-targeted receptor tyrosine kinase inhibitor sunitinib (HY-10255A).
    Thalidomide-NH-C6-NH-Boc
  • HY-112617A
    Thalidomide-O-amido-PEG2-C2-NH2 TFA
    		Inducer 99.72%
    Thalidomide-O-amido-PEG2-C2-NH2 TFA is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 2-unit PEG linker used in PROTAC technology.
    Thalidomide-O-amido-PEG2-C2-NH2 TFA
  • HY-111389
    FAAH-IN-1
    		99.59%
    FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.
    FAAH-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
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