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-114316
    HMG499
    HMG499 is a potent and selective HMG-CoA reductase inhibitor with an IC50 of 0.41 μM. HMG499 can prevent statins-induced accumulation of HMGCR, reduce serum cholesterol levels and decrease atherosclerosis.
    HMG499
  • HY-16715
    Acumapimod
    		99.68%
    Acumapimod (BCT197) is an orally active p38 MAP kinase inhibitor, with an IC50 of less than 1 μM for p38α.
    Acumapimod
  • HY-15888A
    PTC-209 hydrobromide
    		Inducer 99.02%
    PTC-209 hydrobromide is a specific BMI-1 inhibitor with an IC50 of 0.5 μM in HEK293T cell line. PTC-209 hydrobromide irreversibly impairs colorectal cancer-initiating cells (CICs). PTC-209 hydrobromide shows potent anti-myeloma activity and impairs the tumor microenvironment.
    PTC-209 hydrobromide
  • HY-130952
    Thalidomide-O-C8-COOH
    		Inducer
    Thalidomide-O-C8-COOH is the Thalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Thalidomide-O-C8-COOH (Cereblon ligand 3) can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-O-C8-COOH
  • HY-B0151S2
    Pregnenolone-d4-1
    		Inducer 99.34%
    Pregnenolone-d4-1 is the deuterium labeled Pregnenolone. Pregnenolone (3β-Hydroxy-5-pregnen-20-one) is a powerful neurosteroid, the main precursor of various steroid hormones including steroid ketones. Pregnenolone acts as a signaling-specific inhibitor of cannabinoid CB1 receptor, inhibits the effects of tetrahydrocannabinol (THC) that are mediated by the CB1 receptors. Pregnenolone can protect the brain from cannabis intoxication. Pregnenolone is also a TRPM3 channel activator, and also can weakly activate TRPM1 channels.
    Pregnenolone-d<sub>4</sub>-1
  • HY-13260A
    CCT128930 hydrochloride
    		Inducer 98.97%
    CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity.
    CCT128930 hydrochloride
  • HY-107438A
    Thalidomide-O-amido-C4-NH2 hydrochloride
    		Inducer 99.79%
    Thalidomide-O-amido-C4-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs.
    Thalidomide-O-amido-C4-NH2 hydrochloride
  • HY-12956A
    Dinoprost tromethamine salt
    		Inducer 98.0%
    Dinoprost tromethamine salt (Prostaglandin F2α tromethamine salt) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost tromethamine salt is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost tromethamine salt plays a key role in the onset and progression of labour.
    Dinoprost tromethamine salt
  • HY-134591
    Thalidomide-NH-PEG4-COOH
    		Inducer
    Thalidomide-NH-PEG4-COOH is an E3 ligase ligand-linker conjugate which can be used for synthesizing dCBP-1. dCBP-1 is a potent and selective heterobifunctional degrader of p300/CBP.
    Thalidomide-NH-PEG4-COOH
  • HY-14802C
    (+)-Talarozole
    		99.78%
    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
    (+)-Talarozole
  • HY-130951
    Thalidomide-O-C6-COOH
    		Inducer 99.29%
    Thalidomide-O-C6-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C6-COOH
  • HY-100490B
    Rilmenidine phosphate
    		Inducer 99.48%
    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
  • HY-19934
    Pifusertib
    		Inducer 99.81%
    Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy.
    Pifusertib
  • HY-13676R
    Megestrol acetate (Standard)
    		Inhibitor
    Megestrol acetate (Standard) is the analytical standard of Megestrol acetate. This product is intended for research and analytical applications. Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
    Megestrol acetate (Standard)
  • HY-P4808
    PHF6
    		Activator 99.17%
    PHF6 (VQIVYK) is a self-assembly sequence capable of initiating the full-length tau protein aggregation and is mapped to the third microtubule-binding repeat region of the tau protein.
    PHF6
  • HY-B0261S
    Meloxicam-d3
    		Inducer 99.55%
    Meloxicam-d3 is deuterium labeled Meloxicam. Meloxicam is a non-steroidal antiinflammatory agent, inhibits COX activity, with IC50s of 0.49 μM and 36.6 μM for COX-2 and COX-1, respectively.
    Meloxicam-d<sub>3</sub>
  • HY-N6996R
    Methyl Eugenol (Standard)
    		Inducer
    Methyl Eugenol (Standard) is the analytical standard of Methyl Eugenol. This product is intended for research and analytical applications. Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury.
    Methyl Eugenol (Standard)
  • HY-70002R
    Enzalutamide (Standard)
    		Inducer
    Enzalutamide (Standard) is the analytical standard of Enzalutamide. This product is intended for research and analytical applications. Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.
    Enzalutamide (Standard)
  • HY-156966
    ATG12-ATG3 inhibitor 1
    		Inhibitor 98.19%
    ATG12-ATG3 inhibitor 1 (compound 189) is a potent inhibitor of autophage.
    ATG12-ATG3 inhibitor 1
  • HY-B0006S1
    Carvedilol-d4
    		Inducer 99.80%
    Carvedilol-d4 is the deuterium labeled Carvedilol. Carvedilol (BM 14190) is a non-selective β/α-1 blocker. Carvedilol inhibits lipid peroxidation in a dose-dependent manner with an IC50 of 5 μM. Carvedilol is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol is an autophagy inducer that inhibits the NLRP3 inflammasome.
    Carvedilol-d<sub>4</sub>
Cat. No. Product Name / Synonyms Application Reactivity
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