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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. Nombre del producto Efecto Pureza Chemical Structure
  • HY-10999S
    Trametinib-d4
    		Inducer 99.87%
    Trametinib-d4 is the deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
    Trametinib-d<sub>4</sub>
  • HY-B0113S
    Omeprazole-d3
    		98.99%
    Omeprazole-d3 (H 16868-d3) is deuterium labeled Omeprazole. Omeprazole (H 16868) is an orally active H+,K+-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.
    Omeprazole-d<sub>3</sub>
  • HY-17589AS
    Chloroquine-d5
    		Inhibitor 99.90%
    Chloroquine-d5 is deuterium labeled Chloroquine (HY-17589A). Chloroquine is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM).
    Chloroquine-d<sub>5</sub>
  • HY-B0671R
    Vancomycin (Standard)
    		Inhibitor
    Vancomycin (Standard) is the analytical standard of Vancomycin. This product is intended for research and analytical applications. Vancomycin is an antibiotic for the treatment of bacterial infections.
    Vancomycin (Standard)
  • HY-100155
    4-IBP
    		98.90%
    4-IBP is a selective σ₁ receptor agonist with high affinity for the σ₁ receptor (Ki =1.7 nM) and moderate affinity for the σ₂ receptor (Ki = 25.2 nM). 4-IBP can make cancer cells more sensitive to the cytotoxic effects of pro-apoptotic and pro-autophagic compounds. 4-IBP significantly reduces the migration ability of a variety of cancer cells. 4-IBP is mainly used in glioblastoma, non-small cell lung cancer and prostate cancer research.
    4-IBP
  • HY-14541S
    Olanzapine-d3
    		Inducer 99.78%
    Olanzapine-d3 (LY170053-d3) is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-19970
    KM11060
    		98.71%
    KM11060 is a corrector of the F508 deletion (F508del)-cystic fibrosis transmembrane conductance regulator (CFTR) trafficking defect. KM11060 can be used for the research of F508del-CFTR processing defect and development of cystic fibrosis research.
    KM11060
  • HY-109096
    Nidufexor
    		99.67%
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
    Nidufexor
  • HY-128339
    Autogramin-1
    		Inhibitor 99.79%
    Autogramin-1 potently inhibits autophagy induced by either starvation (IC50=0.17 μM) or mTORC1 inhibition (Rapamycin; IC50=0.44 μM).
    Autogramin-1
  • HY-111383
    LX2343
    		Inducer 99.80%
    LX2343 is a BACE1 enzyme inhibitor with an IC50 value of 11.43±0.36 μM. LX2343 acts as a non-ATP competitive PI3K inhibitor with an IC50 of 15.99±3.23 μM. LX2343 stimulates autophagy in its promotion of Aβ clearance.
    LX2343
  • HY-138782
    Thalidomide-Piperazine-PEG1-COOH
    		Inducer 99.24%
    Thalidomide-Piperazine-PEG1-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-Piperazine-PEG1-COOH
  • HY-119936
    GLPG2451
    		99.68%
    GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM.
    GLPG2451
  • HY-138772
    Thalidomide-NH-PEG2-COOH
    		Inducer 99.04%
    Thalidomide-NH-PEG2-COOH is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-NH-PEG2-COOH
  • HY-122694A
    Thalidomide-O-amido-PEG-C2-NH2 hydrochloride
    		Inducer 98.10%
    Thalidomide-O-amido-PEG-C2-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-PEG-C2-NH2 hydrochloride
  • HY-131880
    Thalidomide-O-C2-acid
    		Inducer
    Thalidomide-O-C2-acid is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-C2-acid
  • HY-14648S
    Dexamethasone-d5
    		Inducer 99.23%
    Dexamethasone-d5 is the deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
    Dexamethasone-d<sub>5</sub>
  • HY-B0401S
    Tolbutamide-d9
    		Inducer 99.02%
    Tolbutamide-d9 is the deuterium labeled Tolbutamide. Tolbutamide is a first generation potassium channel blocker, sulfonylurea oral hypoglycemic agent.
    Tolbutamide-d<sub>9</sub>
  • HY-10585S
    Valproic acid-d4
    		Inducer 98.0%
    Valproic acid-d4 is the deuterium labeled Valproic acid. Valproic acid (VPA; 2-Propylpentanoic Acid) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
    Valproic acid-d<sub>4</sub>
  • HY-B1490S
    Imipramine-d4 hydrochloride
    		Inducer 99.95%
    Imipramine-d4 (hydrochloride) is the deuterium labeled Imipramine hydrochloride. Imipramine hydrochloride is an orally active tertiary amine tricyclic antidepressant. Imipramine hydrochloride is a Fascin1 inhibitor with antitumor activities. Imipramine hydrochloride also inhibits serotonin transporter with an IC50 value of 32 nM. Imipramine hydrochloride stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine hydrochloride shows neuroprotective and immunomodulatory effects.
    Imipramine-d<sub>4</sub> hydrochloride
  • HY-10882S
    Clotrimazole-d5
    		Inhibitor 99.47%
    Clotrimazole-d5 is the deuterium labeled Clotrimazole. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
    Clotrimazole-d<sub>5</sub>
Cat. No. Nombre del producto / Synonyms Application Reactivity
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