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-161850
    ULK1-IN-3
    		Inhibitor
    ULK1-IN-3 (Compound 8) is a novel chromone-based as a potential inhibitor of ULK1. ULK1-IN-3 inhibits cell cycle, autophagy and induces apoptosis, oxidative stress in colon cancer cell lines.
    ULK1-IN-3
  • HY-N0112R
    Dihydromyricetin (Standard)
    		Inducer
    Dihydromyricetin (Standard) is the analytical standard of Dihydromyricetin. This product is intended for research and analytical applications. Dihydromyricetin is a potent inhibitor with an IC50 of 48 μM on dihydropyrimidinase. Dihydromyricetin can activate autophagy through inhibiting mTOR signaling. Dihydromyricetin suppresses the formation of mTOR complexes (mTORC1/2). Dihydromyricetin is also a potent influenza RNA-dependent RNA polymerase inhibitor with an IC50 of 22 μM.
    Dihydromyricetin (Standard)
  • HY-121532
    (-)-Rasfonin
    		Inducer
    (-)-Rasfonin is a fungal secondary metabolite and inhibits small G proteins Ras. (-)-Rasfonin induces apoptosis, necrosis and autophagy in ACHN cells (a renal carcinoma cell line).
    (-)-Rasfonin
  • HY-152228
    SMYD3-IN-2
    SMYD3-IN-2 is a SMYD3 inhibitor against gastric cancer via inducing lethal autophagy. SMYD3-IN-2 has inhibitory for SMYD3 and BGC823 cells with IC50 values of 0.81 μM and 0.75 μM, respectively. SMYD3-IN-2 can be used for the research of cancer.
    SMYD3-IN-2
  • HY-B0075R
    Melatonin (standard)
    		Inhibitor
    Melatonin (Standard) is the analytical standard of Melatonin. This product is intended for research and analytical applications. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress.
    Melatonin (standard)
  • HY-14754R
    Salirasib (Standard)
    		Inducer
    Salirasib (Standard) is the analytical standard of Salirasib. This product is intended for research and analytical applications. Salirasib is a Ras inhibitor that inhibits specifically both oncogenically activated Ras and growth factor receptor-mediated Ras activation, resulting in the inhibition of Ras-dependent tumor growth.
    Salirasib (Standard)
  • HY-N0783R
    Eupatilin (Standard)
    		Inducer
    Eupatilin (Standard) is the analytical standard of Eupatilin. This product is intended for research and analytical applications. Eupatilin, a lipophilic flavonoid isolated from Artemisia argyi Lévl. et Van., is a PPARα agonist, and possesses anti-apoptotic, anti-oxidative and anti-inflammatory activities.
    Eupatilin (Standard)
  • HY-N0733S1
    Glucosamine-2-13C hydrochloride
    Glucosamine-2-13C (hydrochloride) is the 13C labeled Glucosamine hydrochloride. Glucosamine hydrochloride (D-Glucosamine hydrochloride) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as
    Glucosamine-2-<sup>13</sup>C hydrochloride
  • HY-100532S
    CD437-13C6
    CD437-13C6 is the 13C- and deuterium labeled CD437. CD437 is a selective Retinoic Acid Receptor γ (RARγ) agonist.
    CD437-<sup>13</sup>C<sub>6</sub>
  • HY-N0231R
    Bavachalcone (Standard)
    		Activator
    Bavachalcone (Standard) is the analytical standard of Bavachalcone. This product is intended for research and analytical applications. Bavachalcone is a potent inducer of apoptosis. Bavachalcone exerts anticancer activity by promoting autophagy and apoptosis in HepG2 cells. Bavachalcone acts as an anti-neuroinflammatory and antidepressant through the NF-κB pathway. Bavachalcone inhibits osteoclasts by interfering with ERK and Akt signaling pathways and the expression of c-Fos and NFATc1. Bavachalcone exhibits a significant inhibitory effect on baculovirus-expressed BACE-1 in vitro.
    Bavachalcone (Standard)
  • HY-170992
    Autophagy agonist-1
    		Agonist
    Autophagy agonist-1 (compound 22) is an Autophagy agonist. Autophagy agonist-1 exhibits significant anticancer activity against HepG2 cells and normal cells with IC50s of 8.8 μM and > 50 μM. Autophagy agonist-1 induces G1/S phase cell cycle arrest and inhibits CDK4 and CyclinD1 expression while upregulating P21. Autophagy agonist-1 promotes the accumulation of autophagosomes and the proteins LC3 and PINK1, enhancing autophagy and mitophagy in HepG2 cells.
    Autophagy agonist-1
  • HY-138850
    Thalidomide-NH-amido-C3-NH2
    		Inducer
    Thalidomide-NH-amido-C3-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-C3-NH2
  • HY-W584521
    Thalidomide-4-NH-PEG1-NH2 TFA
    		Inducer
    Thalidomide-4-NH-PEG1-NH2 TFA is an E3 Ligase Ligand-Linker Conjugate consisting of Thalidomide (HY-14658) and NH-PEG3-NH-Boc. Thalidomide-4-NH-PEG1-NH2 TFA acts as a ligand for Cereblon to recruit CRBN protein. Thalidomide-4-NH-PEG1-NH2 TFA is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-NH2 TFA
  • HY-163136
    Autophagy/REV-ERB-IN-1
    		Inhibitor
    Autophagy/REV-ERB-IN-1 (compound 24) is a dual inhibitor of autophagy and REV-ERB. Autophagy/REV-ERB-IN-1 has anti-tumor activity with a CC50 value of 2.3 μM on BTB-474 cells.
    Autophagy/REV-ERB-IN-1
  • HY-N1372AR
    Fangchinoline (Standard)
    		Inducer
    Fangchinoline (Standard) is the analytical standard of Fangchinoline. This product is intended for research and analytical applications. Fangchinoline is isolated from Stephania tetrandra with extensive biological activities, such as enhancing immunity, anti-inflammatory sterilization and anti-atherosclerosis. Fangchinoline, a novel HIV-1 inhibitor, inhibits HIV-1 replication by impairing gp160 proteolytic processing. Fangchinoline targets Focal adhesion kinase (FAK) and suppresses FAK-mediated signaling pathway in tumor cells which highly expressed FAK. Fangchinoline induces apoptosis and adaptive autophagy in bladder cancer.
    Fangchinoline (Standard)
  • HY-168640
    RIP3 activator 1
    		Inducer
    RIP3 activator 1 (compound C8) is a potent RIP3 activator. RIP3 activator 1 inhibits cell growth. RIP3 activator 1 induces necroptosis through the RIP3/p62/Keap1 signaling pathway. RIP3 activator 1 increases the protein expression of p-MLKL. RIP3 activator 1 induces autophagy. RIP3 activator 1 increases accumulation of LC3-II and p62 protein expression.
    RIP3 activator 1
  • HY-14616R
    Shogaol (Standard)
    		Inducer
    Shogaol (Standard) is the analytical standard of Shogaol. This product is intended for research and analytical applications. Shogaol (-Shogaol), an active compound isolated from Ginger (Zingiber officinale Rosc), exhibits a variety of biological activities including anticancer, anti-inflammation, and anti-oxidation.
    Shogaol (Standard)
  • HY-148114
    MOPIPP
    		Inducer
    MOPIPP is a novel indolebased chalcone, and vacuolin-1, is a non-lethal vacuoleinducing 2-propyl analog of MOMIPP (HY-119624). MOPIPP induces cellular vacuolization and increases autophagosomes numbers. MOPIPP also triggers methuosis, and interrupts glucose uptake and glycolytic metabolism. MOPIPP can cross the blood-brain barrier and shows efficacy in suppressing tumor progression agaisnt glioblastoma cells.
    MOPIPP
  • HY-156348
    MAO-B-IN-26
    		Inhibitor
    MAO-B-IN-26 (Compound IC9) is a MAO-B and acetylcholinesterase inhibitor. MAO-B-IN-26 protects SH?SY5Y cells against Aβ induced cytotoxicity, morphological changes, ROS generation and membrane damage. MAO-B-IN-26 also inhibits Aβ induced autophagy and apoptosis. MAO-B-IN-26 can be used as a neuroprotective agent against Alzheimer’s disease.
    MAO-B-IN-26
  • HY-135564A
    RK-682
    		Inhibitor ≥99.0%
    RK-682 is the inhibitor for protein tyrosine phosphatase (PTPase), heparanase, phospholipase A2 and HIV-1 protease. RK-682 inhibits the dephosphorylation of CD45 (IC50 is 54 μM) and VHR (IC50 is 2.0 μM), and thereby inhibits the ERK signaling pathway. RK-682 inhibits the cell viability of cancer cell MGH-U3, T24 and UROtsa with IC50s of 78.2, 43.2 and 145 nM, respectively, arrests the cell cycle at G1/S phase, inhibits the cell migration and autophagy in MGH-U3 and T24.
    RK-682
Cat. No. Product Name / Synonyms Application Reactivity
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