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-B0968AR
    Trimetazidine (Standard)
    		Inducer
    Trimetazidine (Standard) is the analytical standard of Trimetazidine. This product is intended for research and analytical applications. Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective agent, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
    Trimetazidine (Standard)
  • HY-101491S
    SR-18292-d9
    SR-18292-d9 is the deuterium labeled SR-18292 (HY-101491). SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
    SR-18292-d<sub>9</sub>
  • HY-N0305S2
    5-Aminolevulinic acid-13C hydrochloride
    5-Aminolevulinic acid-13C (hydrochloride) is the 13C labeled 5-Aminolevulinic acid hydrochloride[1]. 5-Aminolevulinic acid hydrochloride (5-ALA hydrochloride) is an intermediate in heme biosynthesis in the body and the universal precursor of tetrapyrroles[2][3].
    5-Aminolevulinic acid-<sup>13</sup>C hydrochloride
  • HY-W654130
    Daunorubicin-13C,d3
    		Inducer
    Daunorubicin-13C,d3 is 13C and deuterium labeled Daunorubicin. Daunorubicin (Daunomycin) is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin inhibits DNA and RNA synthesis. Daunorubicin is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin is also an anthracycline antibiotic. Daunorubicin can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin-<sup>13</sup>C,d<sub>3</sub>
  • HY-B0863B
    Glyphosate isopropylammonium
    		Inducer
    Glyphosate isopropylammonium, a non-selective systemic biocide with broad-spectrum activity, is an herbicidal derivative of the amino acid glycine. Glyphosate isopropylammonium inhibits the enzymatic activity of the 5-endopyruvylshikimate 3-phosphate synthase (EPSPS) in the shikimic acid pathway, preventing the synthesis of the aromatic amino acids tyrosine, phenylalanine, and tryptophan. Glyphosate isopropylammonium induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, processes that lead to neuronal death by autophagia, necrosis, or apoptosis, as well as the appearance of behavioral and motor disorders.
    Glyphosate isopropylammonium
  • HY-B0233R
    Isradipine (Standard)
    		Inducer
    Isradipine (Standard) is the analytical standard of Isradipine. This product is intended for research and analytical applications. Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
    Isradipine (Standard)
  • HY-13518R
    Piceatannol (Standard)
    		Inducer
    Piceatannol (Standard) is the analytical standard of Piceatannol. This product is intended for research and analytical applications. Piceatannol is a well-known Syk inhibitor and reduces the expression of iNOS induced by TNF. Piceatannol is an effective agent for research of acute lung injury (ALI). Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. Piceatannol induces apoptosis in DLBCL cell lines. Piceatannol induces autophagy and apoptosis in MOLT-4 human leukemia cells.
    Piceatannol (Standard)
  • HY-12008A
    Erlotinib mesylate
    		Inducer
    Erlotinib mesylate (CP-358774 mesylate) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib mesylate
  • HY-135811R
    Desethyl chloroquine (Standard)
    		Inhibitor
    Desethyl chloroquine (Standard) is the analytical standard of Desethyl chloroquine. This product is intended for research and analytical applications. Desethyl chloroquine is a major desethyl metabolite of Chloroquine. Chloroquine diphosphate is an inhibitor of autophagy and toll-like receptors (TLRs). Desethyl chloroquine possesses antiplasmodic activity.
    Desethyl chloroquine (Standard)
  • HY-17504BS2
    Rosuvastatin-13C,d3 sodium
    		Inducer
    Rosuvastatin-13C,d3 sodium is 13C and deuterated labeled Rosuvastatin sodium (HY-17504B). Rosuvastatin Sodium is a competitive HMG-CoA reductase (HMGCR) inhibitor, with an IC50 of 11 nM. Rosuvastatin Sodium potently blocks hERG current with an IC50 of 195 nM. Rosuvastatin Sodium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Sodium effectively lowers low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    Rosuvastatin-<sub>13</sub>C,d<sub>3</sub> sodium
  • HY-13777S
    Zoledronic acid-d5
    		Inducer
    Zoledronic acid-d5 is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
    Zoledronic acid-d<sub>5</sub>
  • HY-10181S1
    Dasatinib-d4
    		Inducer
    Dasatinib-d4 (BMS-354825-d4) is deuterium labeled Dasatinib. Dasatinib (BMS-354825) is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib-d<sub>4</sub>
  • HY-13062R
    Daunorubicin (hydrochloride) (Standard)
    		Inducer
    Daunorubicin (hydrochloride) (Standard) is the analytical standard of Daunorubicin (hydrochloride). This product is intended for research and analytical applications. Daunorubicin (Daunomycin) hydrochloride is a topoisomerase II inhibitor with potent anti-tumor activity. Daunorubicin hydrochloride inhibits DNA and RNA synthesis. Daunorubicin hydrochloride is a cytotoxin that inhibits cancer cell viability and induces apoptosis and necrosis. Daunorubicin hydrochloride is also an anthracycline antibiotic. Daunorubicin hydrochloride can be used in the research of infection and variety of cancers, including leukemia, non-Hodgkin lymphomas, Ewing's sarcoma, Wilms' tumor.
    Daunorubicin (hydrochloride) (Standard)
  • HY-W653999
    Glycodeoxycholic acid-d5
    		Inducer
    Glycodeoxycholic acid-d5 is deuterium labeled Glycodeoxycholic Acid. Glycodeoxycholic Acid is a natural product found in Streptomyces nigricans, Trypanosoma brucei and C. elegans. Glycodeoxycholic Acid induces hepatocyte necrosis and autophagy in patients with obstructive cholestasis.
    Glycodeoxycholic acid-d<sub>5</sub>
  • HY-12956R
    Dinoprost (Standard)
    		Inducer
    Dinoprost (Standard) is the analytical standard of Dinoprost. This product is intended for research and analytical applications. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
    Dinoprost (Standard)
  • HY-10218S1
    Everolimus-13C2,d4
    		Inducer
    Everolimus-13C2,d4 (RAD001-13C2,d4) is 13C labeled Everolimus. Everolimus (RAD001) is a Rapamycin (HY-10219) derivative and a potent, selective and orally active mTOR1 inhibitor. Everolimus binds to FKBP-12 to generate an immunosuppressive complex. Everolimus inhibits tumor cells proliferation and induces cell apoptosis and autophagy. Everolimus has potent immunosuppressive and anticancer activities.
    Everolimus-<sup>13</sup>C<sub>2</sub>,d<sub>4</sub>
  • HY-10336R
    Brivanib (alaninate) (Standard)
    		Inducer
    Brivanib (alaninate) (Standard) is the analytical standard of Brivanib (alaninate). This product is intended for research and analytical applications. Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ.
    Brivanib (alaninate) (Standard)
  • HY-10159R
    Nilotinib (Standard)
    		Inducer
    Nilotinib (Standard) is the analytical standard of Nilotinib. This product is intended for research and analytical applications. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib (Standard)
  • HY-10405R
    Pamapimod (Standard)
    Pamapimod (Standard) is the analytical standard of Pamapimod. This product is intended for research and analytical applications. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
    Pamapimod (Standard)
  • HY-W129233
    Dihydroartemisinin (mixture of α and β isomers)
    		Inducer
    Dihydroartemisinin (mixture of α and β isomers) is an anti-malaria and anticancer agent, as well as an active metabolite of artemisinin and its derivatives. Dihydroartemisinin exerts anticancer effects through various molecular mechanisms, such as inhibiting proliferation, inducing apoptosis, inhibiting tumor metastasis and angiogenesis, promoting immune function, inducing autophagy and endoplasmic reticulum stress.
    Dihydroartemisinin (mixture of α and β isomers)
Cat. No. Product Name / Synonyms Application Reactivity
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