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-W012875R
    3-Nitropropanoic acid (Standard)
    3-Nitropropanoic acid (Standard) is the analytical standard of 3-Nitropropanoic acid. This product is intended for research and analytical applications. 3-Nitropropanoic acid (β-Nitropropionic acid) is an irreversible and orally active inhibitor of succinate dehydrogenase. 3-Nitropropanoic acid exhibits potent antimycobacterial activity with a MIC value of 3.3 μM. 3-Nitropropanoic acid can induce cell apoptosis[1][2].
    3-Nitropropanoic acid (Standard)
  • HY-W584522
    Thalidomide-4-NH-PEG1-COO(t-Bu)
    		Inducer
    Thalidomide-4-NH-PEG1-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG1-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-COO(t-Bu)
  • HY-N0107R
    Cyclovirobuxine D (Standard)
    		Inducer
    Cyclovirobuxine D (Standard) is the analytical standard of Cyclovirobuxine D. This product is intended for research and analytical applications. Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR. Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis. Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction.
    Cyclovirobuxine D (Standard)
  • HY-B0228S7
    Adenosine-d-1
    Adenosine-d-1 is the deuterium labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular phys
    Adenosine-d-1
  • HY-10585B
    Valproic acid (sodium)(2:1)
    		Inducer
    Valproic acid (VPA) sodium (2:1) is an orally active 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 sodium (2:1) activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium (2:1) is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid (sodium)(2:1)
  • HY-138856
    Thalidomide-NH-amido-PEG3-C2-NH2
    		Inducer
    Thalidomide-NH-amido-PEG3-C2-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-PEG3-C2-NH2
  • HY-10208S1
    Pazopanib-13C,d3
    Pazopanib-13C,d3 is the deuterium and 13C labeled Pazopanib[1]. Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively[2][3].
    Pazopanib-<sup>13</sup>C,d<sub>3</sub>
  • HY-B0143S4
    Niacin-15N,13C3
    Niacin-15N,13C3 is the 13C and 15N labeled Niacin[1]. Niacin (Vitamin B3) is an orally active water-soluble B3 vitamin that is an essential nutrient for humans. Niacin (Vitamin B3) plays a key role in energy metabolism, cell signaling cascades regulating gene expression and apoptosis. Niacin (Vitamin B3) is also used in the study of cardiovascular diseases[2][3].
    Niacin-<sup>15</sup>N,<sup>13</sup>C<sub>3</sub>
  • HY-N0174R
    Cryptotanshinone (Standard)
    		Inducer
    Cryptotanshinone (Standard) is the analytical standard of Cryptotanshinone. This product is intended for research and analytical applications. Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
    Cryptotanshinone (Standard)
  • HY-163661
    p53-MDM2-IN-5
    		Inducer
    p53-MDM2-IN-5 (compound 5a) is a potent p53-MDM2 inhibitor. p53-MDM2-IN-5 induces apoptosis, autophagy and DNA damage. p53-MDM2-IN-5 induces cell cycle arrest at S and G2/M phases. p53-MDM2-IN-5 shows anti-tumor activity.
    p53-MDM2-IN-5
  • HY-158289
    Isoniazid-KLH
    		Inducer
    Isoniazid-KLH is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
    Isoniazid-KLH
  • HY-N0568R
    Madecassoside (Standard)
    		Inhibitor
    Madecassoside (Standard) is the analytical standard of Madecassoside. This product is intended for research and analytical applications. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity[10]. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
    Madecassoside (Standard)
  • HY-138853
    Thalidomide-NH-amido-C8-NH2
    		Inducer
    Thalidomide-NH-amido-C8-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-C8-NH2
  • HY-12057S1
    Vemurafenib-d7
    		Inducer
    Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively[1][4]. Vemurafenib induces cell autophagy[5].
    Vemurafenib-d<sub>7</sub>
  • HY-161196
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
    		Inducer
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
  • HY-18085S2
    Quercetin-13C3
    		Inducer
    Quercetin-13C3 is the 13C-labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively[1].
    Quercetin-<sup>13</sup>C<sub>3</sub>
  • HY-N0007R
    (E,E)-Bisdemethoxycurcumin (Standard)
    		Inducer
    (E,E)-Bisdemethoxycurcumin (Standard) is the analytical standard of (E,E)-Bisdemethoxycurcumin. This product is intended for research and analytical applications. (E,E)-Bisdemethoxycurcumin ((E,E)-Curcumin III) is a curcumin derivative with anti-inflammatory and anticancer activities.
    (E,E)-Bisdemethoxycurcumin (Standard)
  • HY-14541R
    Olanzapine (Standard)
    		Inducer
    Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) 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 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine (Standard)
  • HY-161874
    RPS6-IN-1
    		Inducer
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-B0492R
    Paroxetine (hydrochloride) (Standard)
    		Inducer
    Paroxetine (hydrochloride) (Standard) is the analytical standard of Paroxetine (hydrochloride). This product is intended for research and analytical applications. Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an GRK2 inhibitor with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
    Paroxetine (hydrochloride) (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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