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-15340
    LG100268
    		99.39%
    LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
    LG100268
  • HY-W018791
    Bifendate
    		Inhibitor 99.92%
    Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR).
    Bifendate
  • HY-75839
    Dronedarone Hydrochloride
    		Inducer 99.99%
    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
    Dronedarone Hydrochloride
  • HY-P2322
    Iturin A
    		Inducer 98.53%
    Iturin A is a cyclic lipid peptide with strong antifungal activity. Iturin A induces ROS explosion and induces apoptosis and autophagy in tumor cells. Iturin A has antitumor activity.
    Iturin A
  • HY-10214
    SNX-2112
    		Inducer 99.49%
    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
  • HY-76847S
    Chenodeoxycholic Acid-d4
    		99.53%
    Chenodeoxycholic Acid-d4 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>4</sub>
  • HY-135318
    NBDHEX
    		Inhibitor 98.56%
    NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
    NBDHEX
  • HY-N1441
    Afzelin
    		Inhibitor 99.62%
    Afzelin (Kaempferol-3-O-rhamnoside)It is a flavonol glycoside that has anti-inflammatory, anti-oxidative stress response, anti-apoptotic, and anti-cardiac cytotoxic effects. AfzelinIt can reduce mitochondrial damage, enhance mitochondrial biosynthesis, and reduce mitochondria-related proteins. Parkinand PTENinduced putative kinase 1 (putative kinase 1)s level. AfzelinCan be improved D-galactosamine(GalN)/LPSSurvival rate of mice treated with doxorubicin prophylaxis (HY-15142A)Induced cardiotoxicity and scopolamine (HY-N0296)-induced neurological injury. AfzelinAlso inhibits asthma and allergies caused by ovalbumin.
    Afzelin
  • HY-N0814
    Phytic acid (50% in water)
    		Activator 99.31%
    Phytic acid (myo-Inositol; hexakis dihydrogen phosphate; Inositol hexaphosphate) is an orally active compound. Phytic acid can be derived from the seeds of legumes. Phytic acid is a [PO4]3- storage depot and precursor for other inositol phosphates and pyrophosphates. Phytic acid attenuates Aβ oligomers and upregulates autophagy protein. Phytic acid can be used in cardiovascular disease, metabolic disease, nervous system disease and cancer research.
    Phytic acid (50% in water)
  • HY-N0103
    Sophocarpine
    		Inducer 99.85%
    Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage.
    Sophocarpine
  • HY-10248
    RAF265
    		Inducer 99.80%
    RAF265 is a potent and orally active RAF/VEGFR2 inhibitor.
    RAF265
  • HY-12014
    SU11274
    		Inducer 98.82%
    SU11274 is a selective Met inhibitor with IC50 of 10 nM, but has no effects on PGDFRβ, EGFR or Tie2.
    SU11274
  • HY-12515A
    Nicardipine hydrochloride
    		Inducer 99.73%
    Nicardipine hydrochloride (YC-93) is a calcium channel blocker with an IC50 of 1 μM for blocking cardiac calcium channels. Nicardipine hydrochloride acts as an agent for chronic stable angina and for controlling blood pressure.
    Nicardipine hydrochloride
  • HY-10344
    AZD 6482
    		Inducer 99.93%
    AZD 6482 (KIN-193) is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
    AZD 6482
  • HY-A0119
    Nitroprusside disodium dihydrate
    		Inducer 99.62%
    Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model.
    Nitroprusside disodium dihydrate
  • HY-N0221
    Daurisoline
    		Inhibitor 99.90%
    Daurisoline is a bis-benzylisoquinoline alkaloid that can be isolated from Menispermum dauricum and Rhizoma Menispermi. Daurisoline exerts a blocking effect on hERG and has antiarrhythmic effects. Daurisoline is a potent autophagy blocker that can be used for the research of cancer.
    Daurisoline
  • HY-122942
    Moracin M
    		Modulator 98.99%
    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
  • HY-13287
    SGI-1776 free base
    		Inducer 99.35%
    SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
    SGI-1776 free base
  • HY-100996
    10074-G5
    		99.63%
    10074-G5 is an inhibitor of c-Myc-Max dimerization with an IC50 of 146 μM.
    10074-G5
  • HY-N0837
    Veratramine
    		Inducer 99.84%
    Veratramine (NSC17821; NSC23880) is an orally active inhibitor of the PI3K/Akt/mTOR signaling pathway and a SIGMAR1 modulator. Veratramine induces autophagic apoptosis of tumor cells, arrests the cell cycle at the G0/G1 phase, and inhibits epithelial-mesenchymal transition (EMT)-related proteins to reduce tumor migration. Veratramine reduces spinal cord and sciatic nerve pathological damage in a neuropathy model by inhibiting SIGMAR1 binding to NMDAR and phosphorylation of NMDAR Ser896. Veratramine has anti-tumor proliferation, apoptosis induction, anti-inflammatory and neuroprotective activities, and can be used in the study of cancers such as liver cancer and osteosarcoma, as well as diabetic peripheral neuropathy.
    Veratramine
Cat. No. Product Name / Synonyms Application Reactivity
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