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-B0394S
    Atropine-d5
    		Inhibitor ≥99.0%
    Atropine-d5 is the deuterium labeled Atropine (sulfate monohydrate). Atropine (Tropine tropate) sulfate monohydrate is a broad-spectrum and competitive muscarinic acetylcholine receptor (mAChR) antagonist with anti-myopia effect.
    Atropine-d<sub>5</sub>
  • HY-123056B
    EAD1 (trihydrochloride)
    		Inhibitor
    EAD1 trihydrochloride is a Chloroquine (HY-17589A) analog with anticancer activity. EAD1 trihydrochloride blocks autophagy, leading to the intracellular accumulation of autophagosome-related proteins LC3-II and p62. EAD1 trihydrochloride induces cancer cell apoptosis and inhibits cancer cell proliferation. EAD1 trihydrochloride can be used in the research of lung cancer and pancreatic cancer.
    EAD1 (trihydrochloride)
  • HY-162100
    MR-2088
    		Inhibitor 99.50%
    MR-2088 is a reversible, ATP-competitive, and selective ULK1/2 inhibitor with pEC50 values of 8.3 and 8.7 respectively. MR-2088 effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with Trametinib (HY-10999) (MEK inhibitor) in vitro. MR-2088 can be used for non-small lung cell cancer (NSCLC) research.
    MR-2088
  • HY-16592R
    Brefeldin A (Standard)
    		Inhibitor
    Brefeldin A (Standard) (BFA (Standard)) is the analytical standard of Rutin. This product is intended for research and analytical applications. Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
    Brefeldin A (Standard)
  • HY-14397S
    Indomethacin-d4
    		Inhibitor 99.78%
    Indomethacin-d4 (Indometacin-d4) is a deuterium labeled Indomethacin. Indomethacin is a potent, blood-brain permeable and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin disrupts autophagic flux by disturbing the normal functioning of lysosomes.
    Indomethacin-d<sub>4</sub>
  • HY-124761
    Poloppin
    		Inhibitor 99.40%
    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-B0532AR
    Trifluoperazine dihydrochloride (Standard)
    		Inhibitor
    Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine dihydrochloride (Standard)
  • HY-N5014
    Liensinine perchlorate
    		Inhibitor 99.67%
    Liensinine perchlorate is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine perchlorate suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine perchlorate activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine perchlorate exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine perchlorate can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke.
    Liensinine perchlorate
  • HY-135564A
    RK-682
    		Inhibitor 99.0%
    RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24.
    RK-682
  • HY-122650
    PHY34
    		Inhibitor 98.43%
    PHY34 is an inhibitor that inhibits ATP6V0A2 and CAS thereby inhibiting autophagy, and has a nanomolar effect. PHY34 inhibits cancer cell growth by inducing apoptosis and inhibits tumor growth in xenograft models. PHY34 can be used for research on high grade serous ovarian cancer.
    PHY34
  • HY-B0260S
    Methylprednisolone-d3
    		Inhibitor
    Methylprednisolone-d3 is the deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone-d<sub>3</sub>
  • HY-117025
    Manzamine A
    		Inhibitor 98.2%
    Manzamine A, an orally active beta-carboline alkaloid, inhibits specifically GSK-3β and CDK-5 with IC50s of 10.2 μM and 1.5 μM, respectively. Manzamine A targets vacuolar ATPases and inhibits autophagy in pancreatic cancer cells. Manzamine A has antimalarial and anticancer activities. Manzamine A also shows potent activity against HSV-1.
    Manzamine A
  • HY-N1441R
    Afzelin (Standard)
    		Inhibitor
    Afzelin (Standard) is the analytical standard of Afzelin. This product is intended for research and analytical applications. Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.
    Afzelin (Standard)
  • HY-10211R
    Tanespimycin (Standard)
    		Inhibitor
    Tanespimycin (Standard) is the analytical standard of Tanespimycin. This product is intended for research and analytical applications. Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin also downregulates the stk38 gene expression.
    Tanespimycin (Standard)
  • HY-17589S1
    Chloroquine-d4 phosphate
    		Inhibitor 98.01%
    Chloroquine-d4 (phosphate) is the deuterium labeled Chloroquine phosphate. Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine-d<sub>4</sub> phosphate
  • HY-P10422
    Multi-Leu peptide
    		Inhibitor
    Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer.
    Multi-Leu peptide
  • HY-N0105R
    Rhein (Standard)
    		Inhibitor
    Rhein (Standard) is the analytical standard of Rhein. This product is intended for research and analytical applications.
    Rhein (Standard)
  • HY-B0260S3
    Methylprednisolone-d7
    		Inhibitor 99.73%
    Methylprednisolone-d7 is deuterium labeled Methylprednisolone. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels.
    Methylprednisolone-d<sub>7</sub>
  • HY-A0067R
    Oxybenzone (Standard)
    		Inhibitor
    Oxybenzone (Standard) is the analytical standard of Oxybenzone. This product is intended for research and analytical applications. Oxybenzone (Benzophenone 3) is a commonly used UV filter in sun tans and skin protectants. Oxybenzone act as endocrine disrupting chemicals (EDCs) and can pass through the placental and blood-brain barriers. Benzophenone-3 impairs autophagy, alters epigenetic status, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.
    Oxybenzone (Standard)
  • HY-12678S
    Entrectinib-d4
    		Inhibitor
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice.
    Entrectinib-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
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