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-B0143S4
    Niacin-15N,13C3
    Niacin-15N,13C3 is the 13C and 15N labeled Niacin. Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases.
    Niacin-<sup>15</sup>N,<sup>13</sup>C<sub>3</sub>
  • HY-183772
    TBC1D2-IN-1
    		Inducer
    TBC1D2-IN-1 is a potent orally active and selective TBC1D2 inhibitor with a Kd of 1.1 μM. TBC1D2-IN-1 selectively inhibits TBC1D2-mediated GTP hydrolysis on RAB7A-GTP, promotes RAB7A accumulation on lysosomal membranes, and induces apoptosis and autophagy. TBC1D2-IN-1 exerts selective antiproliferative activity cancer cells. TBC1D2-IN-1 can be used for the research of cervical carcinoma.
    TBC1D2-IN-1
  • HY-N0174R
    Cryptotanshinone (Standard)
    		Inducer
    Cryptotanshinone (Standard) is the analytical standard of Cryptotanshinone. This product is intended for research and analytical applications. Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
    Cryptotanshinone (Standard)
  • HY-101349A
    L 741742 hydrochloride
    		Inducer
    L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma.
    L 741742 hydrochloride
  • HY-163661
    p53-MDM2-IN-5
    		Inducer
    p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.
    p53-MDM2-IN-5
  • HY-158289
    Isoniazid-KLH
    		Inducer
    Isoniazid-KLH is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Isoniazid-KLH
  • HY-182236
    JRN73958
    		Inducer
    JRN73958 (Reduced scytonemin) is a PI3K/Akt, MAPK, and NF-κB inhibitor found in Nostoc commune. JRN73958 inhibits nitric oxide production, induce reactive oxygen species (ROS) generation, and lead to autophagy. JRN73958 decreases LPS (HY-D1056)/IFNγ-induced PI3K/Akt, MAPK, and NF-κB activity. JRN73958 can be used for the research of leukemia.
    JRN73958
  • HY-138853
    Thalidomide-NH-amido-C8-NH2
    		Inducer
    Thalidomide-NH-amido-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-amido-C8-NH2
  • HY-110067
    VO-OHPic
    		Inhibitor
    VO-OHPic is a reversible, noncompetitive PTEN inhibitor with an human IC50 value of 46 nM. VO-OHPic inhibits PTEN signaling, activates Akt-GSK3β and Nrf-2/HO-1 pathways, induces apoptosis resistance and elevates IL-10 levels. VO-OHPic inhibits autophagy, ferroptosis and oxidative stress. VO-OHPic can be used for the research of acute myocardial infarction, intervertebral disc degeneration, cardiomyopathy and cancer.
    VO-OHPic
  • HY-12057S1
    Vemurafenib-d7
    		Inducer
    Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
    Vemurafenib-d<sub>7</sub>
  • HY-161196
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
    		Inducer
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-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-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
  • HY-N0589S
    Dehydrodiisoeugenol-d4
    		Inhibitor
    Dehydrodiisoeugenol-d4 is the deuterium labeled Dehydrodiisoeugenol (HY-N0589). Dehydrodiisoeugenol is an orally active anti-inflammatory and anti-tumor agent. Dehydrodiisoeugenol inhibits the proliferation of colorectal cancer cells, and induces apoptosis, autophagy, endoplasmic reticulum stress and cell cycle arrest. Dehydrodiisoeugenol also exerts anti-inflammatory effects by inhibiting the activation of NF-κB and the expression of COX-2. Dehydrodiisoeugenol can be used in the research related to colorectal cancer, inflammatory diseases and ulcerative colitis.
    Dehydrodiisoeugenol-d<sub>4</sub>
  • HY-161874
    RPS6-IN-1
    		Inducer
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-B0492R
    Paroxetine hydrochloride (Standard)
    		Inducer
    Paroxetine (hydrochloride) (Standard) is the analytical standard of Paroxetine (hydrochloride). This product is intended for research and analytical applications. Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
    Paroxetine hydrochloride (Standard)
  • HY-17507S1
    Pantoprazole-d3
    		Inhibitor
    Pantoprazole-d3 is deuterium labeled Pantoprazole. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
    Pantoprazole-d<sub>3</sub>
  • HY-B1393R
    Dehydrocholic acid (Standard)
    		Modulator
    Dehydrocholic acid (Dehydrocholate) (Standard) is the analytical standard of Dehydrocholic acid (HY-B1393). This product is intended for research and analytical applications. Dehydrocholic acid (Dehydrocholate) is an orally active hydrocholeretic agent. Dehydrocholic acid modulates Autophagy, reduces serum amylase and lipase levels. Dehydrocholic acid has the effects of promoting choleretic function, protecting the liver, reducing pancreatic damage, and regulating cholesterol metabolism. Dehydrocholic acid can be used in the study of acute biliary pancreatitis and obstructive jaundice.
    Dehydrocholic acid (Standard)
  • HY-10201S4
    Sorafenib-d3 tosylate
    Sorafenib-d3 (Donafenib-d3) tosylate is the deuterium labeled Sorafenib (HY-10201). Sorafenib is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib-d3tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib-d3tosylate induces autophagy and apoptosis. Sorafenib-d3tosylate has anti-tumor activity. Sorafenib is a ferroptosis activator.
    Sorafenib-d<sub>3</sub> tosylate
  • HY-13955R
    Telmisartan (Standard)
    		Inducer
    Telmisartan (Standard) is the analytical standard of Telmisartan. This product is intended for research and analytical applications. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan (Standard)
  • HY-B0627A
    Metformin (glycinate)
    		Inducer
    Metformin (1,1-Dimethylbiguanide) glycinate inhibits the mitochondrial respiratory chain in the liver, leading to AMPK activation and enhancing insulin sensitivity, and can be used in the study of type 2 diabetes. Metformin glycinate exerts central glucose-lowering effects by inhibiting Ras-related protein 1 (Rap1) in SF1 hypothalamic neurons. Metformin glycinate also inhibits liver oxidative stress, nitrosative stress, inflammation, and apoptosis caused by liver ischemia/reperfusion injury. In addition, Metformin glycinate regulates the expression of autophagy-related proteins by activating AMPK and inhibiting the mTOR signaling pathway, thereby inducing tumor cell autophagy and inhibiting the growth of renal cell carcinoma in vitro and in vivo.
    Metformin (glycinate)
  • HY-181742
    ULK1/2-IN-1
    		Inducer
    ULK1/2-IN-1 is a tissue-targeted ULK1/2 inhibitor conjugated to the RGR (CRGRRST) tumor neovasculature-homing peptide. ULK1/2-IN-1 mediates autophagy inhibition and induces cytotoxicity in endothelial cells. ULK1/2-IN-1 can be used for the research of tumor-targeted autophagy inhibitors.
    ULK1/2-IN-1
Cat. No. Product Name / Synonyms Application Reactivity
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