1. Signaling Pathways
  2. Autophagy
  3. Autophagy

Autophagy

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-W741136
    (R)-Colchicine
    Inducer
    (R)-Colchicine is the R-isomer of Colchicine (HY-16569). Colchicine, an orally active alkaloid, is a potent tubulin inhibitor and a microtubule disrupting agent. Colchicine inhibits microtubule polymerization with an IC50 of 3 nM. Colchicine is also a competitive antagonist of the α3 glycine receptors (GlyRs). Colchicine prevents non-steroidal anti-inflammatory drug (NSAID)-induced small intestinal injury by inhibiting activation of the NLRP3 inflammasome. Colchicine has extensive anti-inflammatory, immunosuppressive and strong anti-fibrosis effects and has the potential for gouty arthritis research.
    (R)-Colchicine
  • HY-15202S3
    Binimetinib-d4
    Inhibitor
    Binimetinib-d4 (MEK162-d4) is deuterium labeled Binimetinib. Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
    Binimetinib-d<sub>4</sub>
  • HY-107738R
    Guggulsterone (Standard)
    Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
    Guggulsterone (Standard)
  • HY-10547R
    OSU-03012 (Standard)
    Inducer
    OSU-03012 (Standard) is the analytical standard of OSU-03012 (HY-10547). This product is intended for research and analytical applications. OSU-03012 (AR-12; PDK1 inhibitor AR-12) is a blood-brain permeable PDK-1 inhibitor with an IC50 of 5 μM.
    OSU-03012 (Standard)
  • HY-164014
    9-CCN
    Activator
    9-CCN is a lipid compound that specifically targets macrophages. 9-CCN can be used in the study of cardiovascular and cerebrovascular diseases.
    9-CCN
  • HY-101785R
    eIF4A3-IN-2 (Standard)
    eIF4A3-IN-2 (Standard) is the analytical standard of eIF4A3-IN-2 (HY-101785). This product is intended for research and analytical applications. eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM.
    eIF4A3-IN-2 (Standard)
  • HY-B0372AR
    Bromhexine hydrochloride (Standard)
    Inducer
    Bromhexine (hydrochloride) (Standard) is the analytical standard of Bromhexine (hydrochloride). This product is intended for research and analytical applications. Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
    Bromhexine hydrochloride (Standard)
  • HY-13551AR
    Amsacrine hydrochloride (Standard)
    Inducer
    Amsacrine (hydrochloride) (Standard) is the analytical standard of Amsacrine (hydrochloride). This product is intended for research and analytical applications. Amsacrine hydrochloride (m-AMSA hydrochloride; acridinyl anisidide hydrochloride) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine hydrochloride (Standard)
  • HY-18299AR
    Purvalanol A (Standard)
    Inducer
    Purvalanol A (Standard) is the analytical standard of Purvalanol A. This product is intended for research and analytical applications. Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
    Purvalanol A (Standard)
  • HY-13516R
    Aloperine (Standard)
    Inducer
    Aloperine (Standard) is the analytical standard of Aloperine. This product is intended for research and analytical applications. Aloperine is an alkaloid in sophora plants such as Sophora alopecuroides L, which has shown anti-cancer, anti-inflammatory and anti-virus properties. Aloperine is widely used to treat patients with allergic contact dermatitis eczema and other skin inflammation in China. Aloperine induces apoptosis and autophagy in HL-60 cells.
    Aloperine (Standard)
  • HY-50898BR
    Lapatinib ditosylate monohydrate (Standard)
    Inducer
    Lapatinib (ditosylate monohydrate) (Standard) is the analytical standard of Lapatinib (ditosylate monohydrate). This product is intended for research and analytical applications. Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 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 monohydrate (Standard)
  • HY-103706R
    ROC-325 (Standard)
    Inhibitor
    ROC-325 (Standard) is the analytical standard of ROC-325 (HY-103706). This product is intended for research and analytical applications. ROC-325 is a potent and orally active autophagy inhibitor with a strong anticancer activity. ROC-325 induces the deacidification of lysosomes, accumulation of autophagosomes, and disrupted autophagic flux. ROC-325 also induces renal cell carcinoma apoptosis.
    ROC-325 (Standard)
  • HY-N0441R
    Neferine (Standard)
    Modulator
    Neferine (Standard) is the analytical standard of Neferine. This product is intended for research and analytical applications. Neferine is a major bisbenzylisoquinline alkaloid. Neferine strongly inhibits NF-κB activation.
    Neferine (Standard)
  • HY-10448S
    (E/Z)-Capsaicin-d3
    (E/Z)-Capsaicin-d3 is the deuterium labeled (E/Z)-Capsaicin[1].
    (E/Z)-Capsaicin-d<sub>3</sub>
  • HY-17464R
    Cilostazol (Standard)
    Inducer
    Cilostazol (Standard) is the analytical standard of Cilostazol. This product is intended for research and analytical applications. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM.
    Cilostazol (Standard)
  • HY-10403R
    PH-797804 (Standard)
    PH-797804 (Standard) is the analytical standard of PH-797804 (HY-10403). This product is intended for research and analytical applications. PH-797804 is a ATP-competitive, selective p38α/p38β inhibitor (IC50=26 nM and Ki=5.8 nM for p38α; Ki=40 nM for p38β) and does not inhibit JNK2.
    PH-797804 (Standard)
  • HY-103238R
    RSVA405 (Standard)
    Inducer
    RSVA405 (Standard) is the analytical standard of RSVA405 (HY-103238). This product is intended for research and analytical applications. RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 can also be used for the research of obesity.
    RSVA405 (Standard)
  • HY-13735BR
    Quinacrine hydrochloride hydrate (Standard)
    Inhibitor
    Quinacrine (hydrochloride hydrate) (Standard) is the analytical standard of Quinacrine (hydrochloride hydrate). This product is intended for research and analytical applications. Quinacrine hydrochloride hydrate (Mepacrine hydrochloride hydrate) is an antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine hydrochloride hydrate suppresses NF-κB and activates p53 signaling, which results in the induction of the apoptosis.
    Quinacrine hydrochloride hydrate (Standard)
  • HY-B0113S5
    Omeprazole-d6
    Omeprazole-d6 (H 16868-d6) 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>6</sub>
  • HY-B0098AR
    Doxazosin mesylate (Standard)
    Inducer
    Doxazosin (mesylate) (Standard) is the analytical standard of Doxazosin (mesylate). This product is intended for research and analytical applications. Doxazosin mesylate (UK 33274) is a quinazoline-derivative that selectively antagonizes postsynaptic α1-adrenergic receptors.
    Doxazosin mesylate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity