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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-122942R
    Moracin M (Standard)
    		Modulator
    Moracin M (Standard) is the analytical standard of Moracin M. This product is intended for research and analytical applications. Moracin M is a phenolic component that can be isolated from Mori Cortex, is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity.
    Moracin M (Standard)
  • HY-10572BS
    (Rac)-Efavirenz-d4
    		Inducer
    (Rac)-Efavirenz-d4 is a labelled racemic Efavirenz. 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-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    (Rac)-Efavirenz-d<sub>4</sub>
  • HY-50898AR
    Lapatinib ditosylate (Standard)
    		Inducer
    Lapatinib (ditosylate) (Standard) is the analytical standard of Lapatinib (ditosylate). This product is intended for research and analytical applications. Lapatinib ditosylate (GW572016 ditosylate) is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.
    Lapatinib ditosylate (Standard)
  • HY-N0005S1
    Curcumin-d3
    		Inducer
    Curcumin-d3 (Diferuloylmethane-d3 ) is deuterium labeled Curcumin (HY-N0005). Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
    Curcumin-d<sub>3</sub>
  • HY-13629S
    Etoposide-d3
    		Inducer
    Etoposide-d3 (VP-16-d3) is the deuterium labeled Etoposide (HY-13629). Etoposide (VP-16) is an anti-cancer chemotherapy agent. Etoposide inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy.
    Etoposide-d<sub>3</sub>
  • HY-77813R
    Benzyl isothiocyanate (Standard)
    Benzyl isothiocyanate (Standard) is the analytical standard of Benzyl isothiocyanate. This product is intended for research and analytical applications. Benzyl isothiocyanate is an orally available isothiocyanate with bactericidal, anticancer, antiangiogenic and anthelmintic activities. Benzyl isothiocyanate exerts anticancer functions by regulating multiple signaling pathways, including apoptosis, cell proliferation, cell cycle arrest, metastasis, angiogenesis, and autophagy. In addition, Benzyl isothiocyanate can enhance muscle insulin sensitivity to improve obesity-induced hyperglycemia[1][2][3][4][5][6][7][8][9].
    Benzyl isothiocyanate (Standard)
  • HY-103672R
    AZD7624 (Standard)
    AZD7624 (Standard) is the analytical standard of AZD7624 (HY-103672). This product is intended for research and analytical applications. AZD7624 is an inhaled p38 inhibitor, with potent anti-inflammatory activity.
    AZD7624 (Standard)
  • HY-15597R
    Salinomycin (Standard)
    		Modulator
    Salinomycin (Standard) is the analytical standard of Salinomycin. This product is intended for research and analytical applications. Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin shows selective activity against human cancer stem cells[1][2][3].
    Salinomycin (Standard)
  • HY-12956AR
    Dinoprost tromethamine salt (Standard)
    		Inducer
    Dinoprost (tromethamine salt) (Standard) is the analytical standard of Dinoprost (tromethamine salt). This product is intended for research and analytical applications. 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 (Standard)
  • HY-17589BR
    Chloroquine dihydrochloride (Standard)
    		Inhibitor
    Chloroquine (dihydrochloride) (Standard) is the analytical standard of Chloroquine (dihydrochloride). This product is intended for research and analytical applications. Chloroquine dihydrochloride is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine dihydrochloride is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine dihydrochloride is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro (EC50=1.13 μM)[1][2][3][4].
    Chloroquine dihydrochloride (Standard)
  • HY-W705479
    Pazopanib-d3 hydrochloride
    		Inducer
    Pazopanib-d3 (hydrochloride) (GW786034-d3 (hydrochloride)) is deuterium labeled Pazopanib (Hydrochloride). Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib-d<sub>3</sub> hydrochloride
  • HY-10214R
    SNX-2112 (Standard)
    		Inducer
    SNX-2112 (Standard) is the analytical standard of SNX-2112 (HY-10214). This product is intended for research and analytical applications. SNX-2112 (PF 04928473) is an orally active Hsp90 inhibitor, with a Kd of 16 nM for Hsp90 and IC50s of 30 nM, 30 nM for Hsp90 α and Hsp90 β, also induces Her-2 degradation, and inhibits Grp94 and Trap-1, with IC50s of 10 nM, 4.275 μM and 0.862 μM, respectively. SNX-2112 (PF 04928473) binds Hsp90 isoforms Hsp90α, Hsp90β and Hsp90b1/Grp94 with Kds of 4 nM, 6 nM and 484 nM, respectively.
    SNX-2112 (Standard)
  • HY-10212R
    BIIB021 (Standard)
    		Inducer
    BIIB021 (Standard) is the analytical standard of BIIB021. This product is intended for research and analytical applications. BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively.
    BIIB021 (Standard)
  • HY-B0144AR
    Pitavastatin (Standard)
    Pitavastatin (Standard) is the analytical standard of Pitavastatin. This product is intended for research and analytical applications. Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.
    Pitavastatin (Standard)
  • HY-N2329R
    Piperlongumine (Standard)
    		Inducer
    Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.
    Piperlongumine (Standard)
  • HY-10961R
    Momelotinib (Standard)
    		Inhibitor
    Momelotinib (Standard) is the analytical standard of Momelotinib. This product is intended for research and analytical applications. Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
    Momelotinib (Standard)
  • HY-N6002R
    3'-Hydroxypterostilbene (Standard)
    		Inducer
    3'-Hydroxypterostilbene (Standard) is the analytical standard of 3'-Hydroxypterostilbene (HY-N6002). This product is intended for research and analytical applications. 3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 μM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer.
    3'-Hydroxypterostilbene (Standard)
  • HY-10109R
    AS-605240 (Standard)
    		Inducer
    AS-605240 (Standard) is the analytical standard of AS-605240 (HY-10109). This product is intended for research and analytical applications. AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
    AS-605240 (Standard)
  • HY-50855BR
    Silmitasertib sodium salt (Standard)
    		Inducer
    Silmitasertib (sodium salt) (Standard) is the analytical standard of Silmitasertib (sodium salt). This product is intended for research and analytical applications. Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
    Silmitasertib sodium salt (Standard)
  • HY-10248R
    RAF265 (Standard)
    		Inducer
    RAF265 (Standard) is the analytical standard of RAF265 (HY-10248). This product is intended for research and analytical applications. RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265 (Standard)
Cat. No. Nombre del producto / Synonyms Application Reactivity
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