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-10961
    Momelotinib
    		Inhibitor 98.93%
    Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
    Momelotinib
  • HY-13677
    6-Mercaptopurine
    		Inhibitor 99.93%
    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
  • HY-N0480
    Reserpine
    		Inhibitor 99.92%
    Reserpine is an inhibitor of the vesicular monoamine transporter 2 (VMAT2).
    Reserpine
  • HY-17508
    Clarithromycin
    		Inhibitor 99.90%
    Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K.
    Clarithromycin
  • HY-N0105
    Rhein
    		Inhibitor 99.56%
    Rhein is an anthraquinone compound with anti-inflammatory, antioxidant, and anti-cancer effects[1].
    Rhein
  • HY-118630
    Vacuolin-1
    		Inhibitor 98.54%
    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor. Vacuolin-1 blocks the Ca2+-dependent exocytosis of lysosomes and prevents the release of lysosomal content without affecting the process of resealing. vacuolin‐1 is a potent and selective PIKfyve inhibitor and inhibits late‐stage autophagy by impairing lysosomal maturation. Vacuolin-1 can induce vacuole formation and increase the percentage of enucleated cells.
    Vacuolin-1
  • HY-10882
    Clotrimazole
    		Inhibitor 99.91%
    Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
    Clotrimazole
  • HY-N0567
    Hydroxysafflor yellow A
    		Inhibitor 99.46%
    Hydroxysafflor yellow A (Safflomin A) is a natural product of flavonoids isolated from safflower. Hydroxysafflor yellow A can inhibit cell proliferation and promote apoptosis through the autophagy pathway. Hydroxysafflor yellow A has anti-inflammatory, antioxidant and antitumor effects. Hydroxysafflor yellow A can be used in the study of cardiovascular disease.
    Hydroxysafflor yellow A
  • HY-13228
    YM-201636
    		Inhibitor 98.05%
    YM-201636 is a potent and selective PIKfyve inhibitor with an IC50 of 33 nM. YM-201636 also inhibits p110α with an IC50 of 3.3 μM. YM-201636 inhibits retroviral replication.
    YM-201636
  • HY-10940
    Pifithrin-μ
    		Inhibitor 99.69%
    Pifithrin-μ is an inhibitor of p53 and HSP70, with antitumor and neuroprotective activity.
    Pifithrin-μ
  • HY-13264
    Degrasyn
    		Inhibitor 99.70%
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
    Degrasyn
  • HY-12452
    DPN
    		Inhibitor 99.66%
    DPN (Diarylpropionitrile) is a non-steroidal estrogen receptor β (ERβ) selective ligand, with an EC50 of 0.85 nM. DPN has neuroprotective effects in a number of neurological diseases.
    DPN
  • HY-N0484
    Liensinine
    		Inhibitor 99.97%
    Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.
    Liensinine
  • HY-12855A
    Lys05
    		Inhibitor 99.74%
    Lys05 (Lys01 trihydrochloride) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
    Lys05
  • HY-13417A
    AICAR phosphate
    		Inhibitor 99.97%
    AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
    AICAR phosphate
  • HY-N0568
    Madecassoside
    		Inhibitor 99.58%
    Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
    Madecassoside
  • HY-145752
    HaloPROTAC-E
    		Inhibitor 98.76%
    HaloPROTAC-E is a potent Halo PROTAC degrader that reversibly induces degradation of two Halo-tagged endoplasmic reticulum-localized proteins, SGK3 and VPS34, with a DC50 of 3-10 nM. HaloPROTAC-E significantly and selectively induces degradation of endogenous VPS34 complexes (VPS34, VPS15, Beclin1, and ATG14) labeled with Halo and inhibits autophagy.
    HaloPROTAC-E
  • HY-U00434
    3BDO
    		Inhibitor 99.93%
    3BDO is a IFITM3 modulator and mTOR activator with antiviral and autophagy-inhibiting effects. 3BDO exhibits inhibitory activity against porcine coronaviruses. 3BDO increases the protein abundance of IFITM3, inhibits virus-cell membrane fusion, and blocks viral entry. 3BDO inhibits the entry of transmissible gastroenteritis virus, porcine epidemic diarrhea virus, and porcine respiratory coronavirus into host cells. 3BDO can be used for research on porcine coronavirus infection.
    3BDO
  • HY-N0575
    Pinocembrin
    		Inhibitor 99.68%
    Pinocembrin ((+)-Pinocoembrin) is a flavonoid found in propolis, acts as a competitive inhibitor of histidine decarboxylase, and is an effective anti-allergic agent, with antioxidant, antimicrobial and anti-inflammatory properties.
    Pinocembrin
  • HY-15945
    DBeQ
    		Inhibitor 98.79%
    DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
    DBeQ
Cat. No. Product Name / Synonyms Application Reactivity
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