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-161203
    Thalidomide-azetidine-piperazine-C2-O-C-boc
    		Inducer
    Thalidomide-azetidine-piperazine-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-piperazine-C2-O-C-boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-piperazine-C2-O-C-boc
  • HY-W721119
    7-Methylsulfinylheptyl isothiocyanate
    		Inducer
    7-Methylsulfinylheptyl isothiocyanate is an activator for MAPK signaling pathway, which downregulates the melanogenesis related proteins and suppresses the melanin synthesis in B16-F1 cells. 7-Methylsulfinylheptyl isothiocyanate induces autophagy. 7-Methylsulfinylheptyl isothiocyanate is an inducer for phase II enzyme, which exhibits chemoprotective effect against carcinogen. 7-Methylsulfinylheptyl isothiocyanate can be used as cosmetic ingredient for skin whitening and anti-inflammation.
    7-Methylsulfinylheptyl isothiocyanate
  • HY-183786
    Anticancer agent 327
    		Inducer
    Anticancer agent 327, a fluorescent Andrographolide (HY-N0191) derivative, is an NF-κB p50 inhibitor. Anticancer agent 327 covalently binds to the p50 subunit of NF-κB. Anticancer agent 327 reduces levels of multiple oncogenic p53 proteins via the autophagy/lysosome pathway. Anticancer agent 327 can be used for the research of pancreatic ductal adenocarcinoma (Ex/Em = 488/515 nm)[1].
    Anticancer agent 327
  • HY-161208
    Deoxy-thalidomide-Pip-C-PIP-boc
    		Inducer
    Deoxy-thalidomide-Pip-C-PIP-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-Pip-C-PIP-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Deoxy-thalidomide-Pip-C-PIP-boc
  • HY-P3148
    Astin B
    		Inducer
    Astin B is a orally active and potent cyclic pentapeptide, that can be isolated from Aster tataricus. Astin B has hepatotoxic effects in vitro and in vivo and that hepatic injury was primarily mediated by apoptosis in a mitochondria/caspase-dependent manner. Astin B induces autophagy in L-02 cells, increases LC3-II and decreases p62 expression.
    Astin B
  • HY-122984S1
    Diquat-d12(dibromide) 1
    Diquat-d12 dibromide 1 is the deuterium labeled Diquat dibromide (HY-122984). Diquat dibromide is a comprehensive herbicide. Diquat dibromide increases the production of ROS and triggers mitochondrial Autophagy. Diquat dibromide generates free radicals such as superoxide anions through redox cycles, which induce oxidative stress. Diquat dibromide is cytotoxic, reproductive, and neurotoxic. Diquat dibromide is used in cotton, soybean, and other crops to combat noxious weeds.
    Diquat-d<sub>12</sub>(dibromide) 1
  • HY-13300A
    SR-3677 dihydrochloride
    		Inducer
    SR-3677 dihydrochloride (compound 5) is a potent and selective ROCK-I and ROCK-II inhibitor with an IC50 values of 56 nM and 3 nM.
    SR-3677 dihydrochloride
  • HY-149571
    Thalidomide-5-O-C14-NH2 hydrochloride
    		Inducer
    Thalidomide-5-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C14-NH2 hydrochloride
  • HY-161192
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc
    		Inducer
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-piperidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc
  • HY-N0538S1
    Xylitol-2-13C
    Xylitol-2-13C is the 13C labeled Xylit.
    Xylitol-2-<sup>13</sup>C
  • HY-157548
    Antitumor agent-133
    		Inducer
    Antitumor agent-133 (compound 4d) is a bis-isatin derivative, with activities against Huh1 (IC50=17.13 μM) and Huh7 (IC50=8.27 μM). Antitumor agent-133 induces cell autophagy and inhibits tumor growth through regulation of LC3BII, ATG5 and p62 proteins.
    Antitumor agent-133
  • HY-111843
    Ch55-O-C3-NH2
    Ch55-O-C3-NH2 (RAR ligand 1) is a Ch 55-based ligand, which targets RAR. Ch55-O-C3-NH2 (RAR ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.
    Ch55-O-C3-NH2
  • HY-N10305
    Clionamine B
    Clionamine B is an autophagy stimulating aminosteroid isolated from the sponge Cliona celata. Clionamine B strongly stimulates autophagy in human breast cancer MCF-7 cells.
    Clionamine B
  • HY-N2387R
    Pinosylvin (Standard)
    		Inducer
    Pinosylvin (Standard) is the analytical standard of Pinosylvin. This product is intended for research and analytical applications. Pinosylvin is a pre-infectious stilbenoid toxin isolated from the heartwood of Pinus species, has anti-bacterial activities. Pinosylvin is a resveratrol analogue, can induce cell apoptosis and autophapy in leukemia cells.
    Pinosylvin (Standard)
  • HY-154842
    S-Gem
    		Inducer
    S-Gem is a TrxR-dependent prodrug of Gemcitabine (HY-17026) and selectively activated by TrxR. S-Gem shows less cytotoxicity compared to Gemcitabine.
    S-Gem
  • HY-165539
    SMER10
    		Inducer
    SMER10 is a small-molecule enhancer that can induce autophagy. SMER10 can increase the number of EGFP-LC3 positive autophagosoms in COS-7 and HeLa cells, promoting the conversion of LC3-I to autophagosome-associated LC3-II. SMER10 can efficiently promote the degradation of autophagy substrates, including the mutant huntingtin protein (EGFP-HDQ74) associated with Huntington's disease and the A53T α-synuclein protein associated with Parkinson's disease. SMER10 exerts neuroprotective effect.
    SMER10
  • HY-N0164R
    Matrine (Standard)
    		Modulator
    Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI).
    Matrine (Standard)
  • HY-149717
    Antitumor agent-122
    Antitumor agent-122 (Compound 5j) is an antitumor agent with good efficacy, limited toxicity and low resistance. Antitumor agent-122 has antiproliferative activity for MGC-803 cell, HepG2 cell, SKOV3 cell and T24 cell with IC50 values of 5.23 μM, 3.60 μM, 1.43 μM, 3.03 μM, respectively.
    Antitumor agent-122
  • HY-N1416R
    Pogostone (Standard)
    		Inducer
    Pogostone (Standard) is the analytical standard of Pogostone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-163225
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc
    		Inducer
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc
Cat. No. Product Name / Synonyms Application Reactivity
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