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-12048R
    Chelerythrine chloride (Standard)
    		Inducer
    Chelerythrine (chloride) (Standard) is the analytical standard of Chelerythrine (chloride). This product is intended for research and analytical applications. Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy.
    Chelerythrine chloride (Standard)
  • HY-179003
    mTOR/GLS1-IN-1
    		Inducer
    mTOR/GLS1-IN-1 is a potent dual targeted mTOR/GLS1 inhibitor. Has anti proliferative activity against various tumor cells, such as MDA-MB-231 (IC90 = 2.14 µM), MCF-7 (IC90 = 0.91 µM), SK-BR-3 (IC90 = 0.84 µM), and 4T1 (IC90 = 0.32 µM) cells. mTOR/GLS1-IN-1 dose dependently induces ROS accumulation, induces autophagosome formation, and induces apoptosis. mTOR/GLS1-IN-1 can increase Fe2+, decrease GPX4, and induce ferroptosis. mTOR/GLS1-IN-1 can inhibit cell migration, invasion, and angiogenesis. mTOR/GLS1-IN-1 can be used in the research of cancer, such as breast cancer.
    mTOR/GLS1-IN-1
  • HY-15025AR
    Sildenafil citrate (Standard)
    		Inducer
    Sildenafil (citrate) (Standard) is the analytical standard of Sildenafil (citrate). This product is intended for research and analytical applications. Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
    Sildenafil citrate (Standard)
  • HY-124451
    2-Chloronaphthalene
    		Inducer 99.69%
    2-Chloronaphthalene, serving as an intermediate in organic synthesis, is classified as a persistent organic pollutant. 2-Chloronaphthalene can induce apoptosis and autophagy, while inhibiting cell proliferation. 2-Chloronaphthalene leads to cell death through the interplay between autophagy and apoptosis.
    2-Chloronaphthalene
  • HY-139544
    Thalidomide-5-propoxyethanamine
    		Inducer
    Thalidomide-5-propoxyethanamine is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.
    Thalidomide-5-propoxyethanamine
  • HY-B0965AR
    Thioridazine (Standard)
    		Inducer
    Thioridazine (Standard) is the analytical standard of Thioridazine. This product is intended for research and analytical applications. Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine (Standard)
  • HY-163239
    (R)-Thalidomide-piperazine-pyrrolidineethanol
    		Inducer
    (R)-Thalidomide-piperazine-pyrrolidineethanol is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (R)-Thalidomide-piperazine-pyrrolidineethanol can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (R)-Thalidomide-piperazine-pyrrolidineethanol
  • HY-50896S1
    Erlotinib-13C6
    		Inducer
    Erlotinib-13C6 is a 13C-labeled Erlotinib. Erlotinib is a directly acting EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR.
    Erlotinib-<sup>13</sup>C<sub>6</sub>
  • HY-170998
    ATG16L1 stabilizer-1
    		Inducer
    ATG16L1 stabilizer-1 (compound A3B) is an FKBP12-independent ATG16L1 stabilizer that promotes cellular Autophagy. ATG16L1 stabilizer-1 inhibits ATG16L1 with an EC50 of 12.1 μM in the presence or absence of FKBP12. ATG16L1 stabilizer-1 alone induces GFP-LC3 puncta formation to a small extent with an EC50 of 12.0 μM.
    ATG16L1 stabilizer-1
  • HY-N15226
    Butyrolactone Ia
    		Modulator
    Butyrolactone Ia is the inhibitor for the NO production with an IC50 of 18 μM. Butyrolactone Ia inhibits LPS (HY-D1056)-induced mRNA expression of iNOS and the inflammatory cytokine IL-1β. Butyrolactone Ia modulates autophagy in HeLa cells, and exhibits immune suppressive activity.
    Butyrolactone Ia
  • HY-141813
    Autophagy-IN-C1
    		Inhibitor
    Autophagy-IN-C1 not only induces apoptosis but also blocks autophagy in hepatocellular carcinoma (HCC) cells.
    Autophagy-IN-C1
  • HY-N6038R
    Gartanin (Standard)
    Gartanin (Standard) is the analytical standard of Gartanin. This product is intended for research and analytical applications. Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells.
    Gartanin (Standard)
  • HY-158775
    Ferroptocide
    		Inducer
    Ferroptocide is a cell death inducer that triggers ferroptosis and has anti-tumor activity. Ferroptocide can induce oxidative stress, leading to G2/M cell cycle arrest and apoptosis activation in LNCaP cells, while also effectively inhibiting the cell viability of both LNCaP and TRAMP-C1 cells. Ferroptocide can be used to study its capability to induce mitochondrial autophagy and to trigger immunogenic cell death (ICD) in prostate cancer cells.
    Ferroptocide
  • HY-N0692R
    Schisandrol B (Standard)
    		Inducer
    Schisandrol B (Standard) is the analytical standard of Schisandrol B. This product is intended for research and analytical applications. Schisandrol B (Gomisin-A) is a major active constituent of Schisandra chinensis with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities.
    Schisandrol B (Standard)
  • HY-122888
    MPT0L145
    		Inhibitor
    MPT0L145 is a PIK3C3/FGFR inhibitor, with a Kd value of 0.53 nM for PIK3C3. MPT0L145 decreases the phosphorylation of FGFR1, FGFR3 and their downstream proteins (FRS2, ERK and Akt). MPT0L145 induces G0/G1 cell cycle arrest and decreased protein levels of cyclin E. MPT0L145 promotes mitochondrial dysfunction, ROS production, and DNA damage. MPT0L145 is an autophagy inhibitor. MPT0L145 significantly sensitizes cancer cells to targeted or chemotherapeutic agents. MPT0L145 can be used for cancer research, such as bladder cancer and NSCLC.
    MPT0L145
  • HY-B0495S
    Lamotrigine-13C3,d3
    		Inducer
    Lamotrigine-13C3,d3 is the 13C-labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy,?focal seizure, et al.
    Lamotrigine-<sup>13</sup>C<sub>3</sub>,d<sub>3</sub>
  • HY-149568
    Thalidomide-5-O-C11-NH2 hydrochloride
    		Inducer
    Thalidomide-5-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C11-NH2 hydrochloride
  • HY-76847S1
    Chenodeoxycholic Acid-d9
    Chenodeoxycholic Acid-d9 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>9</sub>
  • HY-N10611
    Elsinochrome A
    		Inducer
    Elsinochrome A is a perylene quinone photosensitizer, and can generate reactive oxygen species (ROS) to induce apoptosis and autophagy under light excitation. Elsinochrome A also shows antifungal activity against C. albicans biofilm through photodynamic antimicrobial chemotherapy (PACT). Elsinochrome A can be used for research of photodynamic therapy (PDT) (Ex: 460 nm).
    Elsinochrome A
  • HY-168892
    LC3B recruiter 2
    LC3B recruiter 2 (34R) is an LC3B recruiter and a component of the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), which directly binds to LC3B. LC3B recruiter 2 binds to CDK9 inhibitor SNS-032 (HY-10008) through a linker, forming an ATTEC that targets the degradation of the CDK9 and Cyclin T1 complex (with inhibitory effects on both). Therefore, LC3B recruiter 2 exerts activity through the LC3B-dependent autophagy-lysosome pathway, interfering with the cell cycle of cancer cells, thus exhibiting antitumor activity.
    LC3B recruiter 2
Cat. No. Product Name / Synonyms Application Reactivity
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