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-182054
    Topoisomerase ll/ME-1-IN-1
    		Activator
    Topoisomerase ll/ME-1-IN-1 (Compound 7a) is a Topoisomerase ll and ME-1 inhibitor with an IC50 of 5.03 μM against Topoisomerase ll. Topoisomerase ll/ME-1-IN-1 functionally inhibits the activity of Topoisomerase II and functionally blocks the activity of ME-1. Topoisomerase ll/ME-1-IN-1 induces Autophagy by upregulating the expression of Beclin-1 and LC3-II. Topoisomerase ll/ME-1-IN-1 promotes Apoptosis. Topoisomerase ll/ME-1-IN-1 exhibits antiproliferative activity against breast cancer cells and shows no toxicity to normal mammary epithelial cells. Topoisomerase ll/ME-1-IN-1 can be used in studies related to breast cancer (including triple-negative breast cancer).
    Topoisomerase ll/ME-1-IN-1
  • HY-P10853
    Bacilotetrin C analogue
    		Inducer
    Bacilotetrin C analogue is cytotoxic to triple-negative breast cancer cell line MDA-MB-231 with an IC50 of 0.48 μM. Bacilotetrin C analogue can induce tumor cell autophagy and has anti-tumor activity.
    Bacilotetrin C analogue
  • HY-100490BR
    Rilmenidine phosphate (Standard)
    		Inducer
    Rilmenidine (phosphate) (Standard) is the analytical standard of Rilmenidine (phosphate). This product is intended for research and analytical applications. Rilmenidine phosphate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine phosphate is an alpha 2-adrenoceptor agonist. Rilmenidine phosphate induces autophagy. Rilmenidine phosphate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine phosphate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine phosphate (Standard)
  • HY-N2365R
    Macamide B (Standard)
    Macamide B (Standard) is the analytical standard of Macamide B. This product is intended for research and analytical applications. Macamide B (N-Benzylhexadecanamide; Macamide 1) is a macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH).
    Macamide B (Standard)
  • HY-B0532S
    Trifluoperazine-d8
    		Inhibitor
    Trifluoperazine-d8 is a deuterium labeled Trifluoperazine. Trifluoperazine is an antipsychotic phenothiazine agent and a selective α1-adrenergic receptor antagonist. Trifluoperazine is also a potent dopamine D2 receptor inhibitor .
    Trifluoperazine-d<sub>8</sub>
  • HY-N0213R
    Peiminine (Standard)
    		Inducer
    Peiminine (Standard) is the analytical standard of Peiminine. This product is intended for research and analytical applications. Peiminine is a compound that can be isolated from Bolbostemma paniculatum (Maxim) Franquet (Cucurbitaceae family). Peiminine can induce apoptosis in human hepatocellular carcinoma HepG2 cells through both extrinsic and intrinsic apoptotic pathways. Peiminine has anti-inflammatory, anticancer, anti-osteoporosis, cardioprotective and other activities in many animal models.
    Peiminine (Standard)
  • HY-10572B
    (Rac)-Efavirenz
    		Inducer
    (Rac)-Efavirenz is the isomer of Efavirenz (HY-10572). Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture.
    (Rac)-Efavirenz
  • HY-131874
    Thalidomide-O-C7-acid
    		Inducer 98.55%
    Thalidomide-O-C7-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide (HY-14658) based cereblon ligand and a linker used in PROTAC technology. Thalidomide-O-C7-acid can be used to synthesize PROTAC.
    Thalidomide-O-C7-acid
  • HY-155257
    Thalidomide-5-PEG7-NH2 hydrochloride
    		Inducer 98.79%
    Thalidomide-5-PEG7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-PEG7-NH2 hydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
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