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-12678S1
    Entrectinib-d8
    		Inducer 99.82%
    Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.
    Entrectinib-d<sub>8</sub>
  • HY-14393R
    Emodin (Standard)
    		Inhibitor
    Emodin (Standard) is the analytical standard of Emodin. This product is intended for research and analytical applications. Emodin (Frangula emodin), an anthraquinone derivative, is an anti-SARS-CoV compound. Emodin blocks the SARS coronavirus spike protein and angiotensin-converting enzyme 2 (ACE2) interaction. Emodin inhibits casein kinase-2 (CK2). Anti-inflammatory and anticancer effects. Emodin is a potent selective 11β-HSD1 inhibitor with the IC50 of 186 and 86 nM for human and mouse 11β-HSD1, respectively. Emodin ameliorates metabolic disorder in diet-induced obese mice.
    Emodin (Standard)
  • HY-163199
    ASCT2-IN-2
    		Inducer 99.10%
    ASCT2-IN-2 (compound 25e) is an ASCT2 inhibitor with IC50 of 5.14 μM. ASCT2-IN-2 regulates amino acid metabolism as well as mTOR signaling and thereby induces cell apoptosis. ASCT2-IN-2 inhibits tumor growth.
    ASCT2-IN-2
  • HY-158329
    Alloc-DOX
    		Inducer 98.40%
    Alloc-DOX (N-Alloc doxorubicin) is a Doxorubicin (HY-15142A) prodrug. The combination of a catalyst (such as nano-palladium) and alloc-DOX leads to a decrease in cell viability and tumour growth.
    Alloc-DOX
  • HY-B0284R
    Nifedipine (Standard)
    		Inducer
    Nifedipine (Standard) is the analytical standard of Nifedipine. This product is intended for research and analytical applications. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
    Nifedipine (Standard)
  • HY-125927
    8-Aminoadenosine
    		Inducer 99.05%
    8-Aminoadenosine (8-NH2-Ado), a RNA-directed nucleoside analogue, reduces cellular ATP levels and inhibits mRNA synthesis. 8-Aminoadenosine blocks Akt/mTOR signaling and induces autophagy and apoptosis in a p53-independent manner. 8-Aminoadenosine has antitumor activity.
    8-Aminoadenosine
  • HY-N8418
    Cearoin
    		Inducer 99.09%
    Cearoin increases autophagy and apoptosis through the production of ROS and the activation of ERK.
    Cearoin
  • HY-N0197R
    Baicalin (Standard)
    		Inducer
    Baicalin (Standard) is the analytical standard of Baicalin. This product is intended for research and analytical applications. Baicalin, as a flavonoid glycoside, is an allosteric carnitine palmityl transferase 1 (CPT1) activator. Baicalin reduces the expression of NF-κB.
    Baicalin (Standard)
  • HY-15758R
    3,3'-Diindolylmethane (Standard)
    		Inhibitor
    3,3'-Diindolylmethane (Standard) is the analytical standard of 3,3'-Diindolylmethane. This product is intended for research and analytical applications. 3,3'-Diindolylmethane is a strong, pure androgen receptor (AR) antagonist.
    3,3'-Diindolylmethane (Standard)
  • HY-146349
    PROTAC EGFR degrader 4
    		99.70%
    PROTAC EGFR degrader 4 is a potent PROTAC targeting mutant EGFR.PROTAC EGFR degrader 4 induces EGFRdel19 and EGFRL858R/T790M degradation with DC50s of 0.51 and 126 nM, respectively. PROTAC EGFR degrader 4 significantly inhibits growth of HCC827 and H1975 cell lines with IC50s of 0.83 and 203.1 nM, respectively. Induced EGFR degradation is related to autophagy.
    PROTAC EGFR degrader 4
  • HY-N1988
    Cucurbitacin IIa
    		Inducer 99.90%
    Cucurbitacin IIa (Hemslecin A) is an orally active, blood-brain barrier-permeable EGFR inhibitor with an IC50 of 1.455 nM against human EGFR. Cucurbitacin IIa induces caspase-3-dependent apoptosis, downregulates survivin expression, enhances autophagy levels, disrupts the actin cytoskeleton via actin aggregation, arrests the cell cycle at the G2/M phase, and exerts anti-inflammatory activity by inhibiting the EGFR-MAPK signaling pathway. Cucurbitacin IIa can be used in the research of inflammation-related diseases, depression, and cancers such as non-small cell lung cancer.
    Cucurbitacin IIa
  • HY-13757AS
    Tamoxifen-d5
    		Inducer 99.77%
    Tamoxifen-d5 is a deuterium labeled Tamoxifen. Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM). Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
    Tamoxifen-d<sub>5</sub>
  • HY-10162S1
    Olaparib-d8
    		Inducer 99.88%
    Olaparib-d8 (AZD2281-d8) is the deuterium labeled Olaparib (HY-10162). Olaparib is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
    Olaparib-d<sub>8</sub>
  • HY-15654S
    Phenylbutyrate-d11 sodium
    		Inducer 99.85%
    Phenylbutyrate-d11 (sodium) is deuterium labeled Sodium 4-phenylbutyrate. Sodium 4-phenylbutyrate (4-PBA sodium) is an inhibitor of HDAC and endoplasmic reticulum (ER) stress, used in cancer and infection research.
    Phenylbutyrate-d<sub>11</sub> sodium
  • HY-123581
    Quinocetone
    		Inducer 98.25%
    Quinocetone is an orally active animal feed additive used to increase the meat production of livestock and poultry. Quinocetone exhibits antibacterial activity against a variety of pathogenic microorganisms. Quinocetone exhibits tissue-specific (liver, lymphocyte) toxicity. Quinocetone induces autophagy in cells through the ATF6/DAPK1 pathway. Quinocetone activates the NF-κB and iNOS pathways, leading to cell apoptosis, hepatocyte vacuolar degeneration and fibrosis. Quinocetone can inhibit Nrf2/HO-1 and induce the generation of reactive oxygen species (ROS), leading to oxidative stress and DNA damage.
    Quinocetone
  • HY-W923189
    Neral
    		Inducer
    Neral is a plant-derived anti-inflammatory, antioxidant and anticancer agent. Neral inhibits the phosphorylation of ERK1/2, p38 MAPK and IκB in macrophages induced by LPS (HY-D1056), suppresses the secretion of TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2 in cells, and reduces the production of ROS in cells. Neral inhibits the activation of the NLRP3 inflammasome, and decreases the activation of caspase-1 and the secretion of IL-1β in mouse macrophages. Neral induces autophagy, and exhibits antiproliferative activity both in in vitro breast cancer cell models and mouse xenograft models. Neral regulates brassinosteroid, jasmonic acid and ethylene signaling pathways, and induces the expression of AP2/ERF-ERF and bHLH family genes in rice roots. Neral acts as a herbicide safener, alleviates the damage induced by Fenoxaprop-P-ethyl (HY-B2013), and promotes the elongation of rice roots. Neral can be used in research related to breast cancer, inflammatory and immune system diseases, and herbicide safeners.
    Neral
  • HY-13669R
    Lomustine (Standard)
    		Inducer
    Lomustine (Standard) is the analytical standard of Lomustine. This product is intended for research and analytical applications. Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity.
    Lomustine (Standard)
  • HY-119357
    TN-16
    		Inhibitor 99.78%
    TN-16 is a Microtubule polymerization inhibitor. TN-16 induces G2/M cell cycle arrest, metaphase mitotic arrest and Apoptotic cell death in cells, and blocks late Autophagic flux by inhibiting autophagosome-lysosome fusion. TN-16 suppresses tumor growth in syngeneic mouse breast cancer models. TN-16 can be used in research related to neuroblastoma, cervical cancer, breast cancer and other tumors.
    TN-16
  • HY-176835
    PNR-3-80
    		Inhibitor 98.63%
    PNR-3-80 is an endonuclease G (ENDOG) inhibitor with an IC50 of 0.67 μM. As a non-competitive binder to the ENDOG-substrate complex, PNR-3-80 specifically inhibits the endonuclease activity of ENDOG. PNR-3-80 reduces cell death induced by Cisplatin (HY-17394) and Docetaxel (HY-B0011), and inhibits DNA damage and autophagy (autophagy) induced by Etoposide (HY-13629). PNR-3-80 can be used in studies related to cell injury.
    PNR-3-80
  • HY-N1416
    Pogostone
    		Inducer 99.81%
    Pogostone is isolated from patchouli oil with anti-bacterial and anti-cancer activities. Pogostone inhibits both gram negative and gram positive bacteria, also show inhibitory effect on corynebacterium xerosis with a MIC value of 0.098 µg/ml . Pogostone induces cell apoptosis and autophagy.
    Pogostone
Cat. No. Product Name / Synonyms Application Reactivity
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