1. Autophagy
  2. Autophagy

Autophagy

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.

Autophagy Related Products (2788):

Cat. No. Product Name Effect Purity
  • HY-17394
    Cisplatin Inducer
    Cisplatin (CDDP) is an antineoplastic chemotherapy agent by cross-linking with DNA and causing DNA damage in cancer cells. Cisplatin activates ferroptosis and induces autophagy[1][2][3].
  • HY-10219
    Rapamycin Inducer
    Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1[1]. Rapamycin is an autophagy activator, an immunosuppressant[2].
  • HY-13259
    MG-132 Inducer
    MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis[1][2][3].
  • HY-13757A
    Tamoxifen Inducer 99.92%
    Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells[1][2][3]. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively[5]. Tamoxifen activates autophagy and induces apoptosis[4]. Tamoxifen also can induce gene knockout of CreER transgenic mouse[6].
  • HY-17589A
    Chloroquine Inhibitor 99.50%
    Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
  • HY-B1000R
    Selenomethionine (Standard) Inducer
    Selenomethionine (Standard) is the analytical standard of Selenomethionine. This product is intended for research and analytical applications. Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity[1][2][3].
  • HY-129578R
    Asperphenamate (Standard) Inducer
    Asperphenamate (Standard) is the analytical standard of Asperphenamate. This product is intended for research and analytical applications. Asperphenamate, a fungal metabolite of Aspergillus flatiipes with anti-cancer effect, exhibits IC50 values of 92.3 μM, 96.5 μM and 97.9 μM in T47D, MDA-MB-231 and HL-60 cells, respectively[1][2].
  • 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)[1][2][3][4].
  • HY-B0863S2
    Glyphosate-d2-1
    Glyphosate-d2-1 is the deuterium labeled Glyphosate[1]. Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants[2].
  • HY-W584518
    Thalidomide-5-O-CH2-COOH Inducer
    Thalidomide-5-O-CH2-COOH is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-5-O-CH2-COOH acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-5-O-CH2-COOH is a key intermediate in the synthesis of PROTAC molecules designed based on CRBN.
  • HY-14249
    Bicalutamide Inducer
    Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer[1].
  • HY-18085
    Quercetin Inducer
    Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
  • HY-115570A
    (Z/E)-GW406108X Inhibitor
    (Z/E)-GW406108X is a mixture of different configurations of GW406108X (HY-115570). GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM[1].
  • HY-100587R
    D-Glutamine (Standard) Inducer
    D-Glutamine (Standard) is the analytical standard of D-Glutamine. This product is intended for research and analytical applications. D-Glutamine is a cell-permeable D type stereoisomer of Glutamine.
  • HY-15465A
    KN-93 hydrochloride 99.64%
    KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
  • HY-10261S
    Afatinib-d6 Inducer
    Afatinib-d6 is deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor[1].
  • HY-41547
    Thalidomide 4-fluoride Inducer
    Thalidomide 4-fluoride (Cereblon ligand 4) is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide 4-fluoride (Cereblon ligand 4) can be connected to the ligand for IRAK4 protein by a linker to form PROTAC IRAK4 degrader-1 (HY-129966)[1].
  • HY-141882
    DC-LC3in-D5 Inhibitor 98.62%
    DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy[1].
  • HY-10225
    Belinostat Inducer 99.95%
    Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts.
  • HY-N0853
    Alisol A Inducer
    Alisol A is a natural product.