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-13270A
    ABT-751 hydrochloride
    		Inducer
    ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer.
    ABT-751 hydrochloride
  • HY-168843
    PSP205
    		Inducer
    PSP205 is a potent anticancer agent. PSP205 shows cytotoxicity. PSP205 induces apoptosis. PSP205 induces ER-stress-mediated autophagy. PSP205 increases the protein expression of LC3BII and increases the CHOP and spliced XBP1 at the mRNA and protein levels.
    PSP205
  • HY-W794759
    Valproic acid magnesium
    		Inducer
    Valproic acid magnesium (Magnesium valproate) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid magnesium inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid magnesium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid magnesium is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid magnesium
  • HY-N0370S
    Bergapten-d3
    		Inducer
    Bergapten-d3 is deuterium labeled Bergapten. Bergapten is a natural anti-inflammatory and anti-tumor agent. Bergapten is inhibitory towards mouse and human CYP isoforms.
    Bergapten-d<sub>3</sub>
  • HY-N0735R
    Phellodendrine chloride (Standard)
    Phellodendrine chloride (Standard) is the analytical standard of Phellodendrine chloride (HY-N0735). Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway.
    Phellodendrine chloride (Standard)
  • HY-12542R
    Dantrolene (Standard)
    		Inducer
    Dantrolene (Standard) is the analytical standard of Dantrolene. This product is intended for research and analytical applications. Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
    Dantrolene (Standard)
  • HY-32736R
    Triptonide (Standard)
    		Inducer
    Triptonide (Standard) is the analytical standard of Triptonide. This product is intended for research and analytical applications. Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.
    Triptonide (Standard)
  • HY-181936
    Atg4B activator-1
    		Inducer
    Atg4B activator-1 (Compound 16a) is an allosteric, selective, and orally active ATG4B activator with a Kd of 0.2199 μM. Atg4B activator-1 binds to the allosteric pocket of ATG4B and induces conformational changes. Atg4B activator-1 induces Autophagy. Atg4B activator-1 inhibits the proliferation and migration of triple-negative breast cancer cells. Atg4B activator-1 can be used in studies related to triple-negative breast cancer.
    Atg4B activator-1
  • HY-138848
    Thalidomide-4-O-C5-NH2
    		Inducer
    Thalidomide-4-O-C5-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-4-O-C5-NH2
  • HY-N0417R
    Cucurbitacin E (Standard)
    		Inducer
    Cucurbitacin E (Standard) is the analytical standard of Cucurbitacin E. This product is intended for research and analytical applications. Cucurbitacin E is a natural compound which from Cucurbitaceae plants. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
    Cucurbitacin E (Standard)
  • HY-139549
    Thalidomide-benzo
    		Inducer
    Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-benzo
  • HY-170989
    BRD4 degrader-5
    		Inducer
    BRD4 degrader-5 (Compound 23) is a hydrophobic tag (HyTag)-based protein degrader for BRD4 (DC50 = 24.7 μM) through ER stress and autophagy-lysosome pathway. BRD4 degrader-5 inhibits the proliferation of cancer cell 4T1 with an IC50 of 20.6 μM.
    BRD4 degrader-5
  • HY-17356G
    Fenofibrate (GMP)
    		Inducer
    Fenofibrate (GMP) is Fenofibrate (HY-17356) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
    Fenofibrate (GMP)
  • HY-B0284S1
    Nifedipine-d4
    		Inducer
    Nifedipine-d4 is the deuterium labeled Nifedipine. Nifedipine (BAY-a-1040) is a potent calcium channel blocker and agent of choice for cardiac insufficiencies.
    Nifedipine-d<sub>4</sub>
  • HY-B0495S3
    Lamotrigine-13C2,15N
    Lamotrigine-13C2,15N is the 13C and 15N labeled Lamotrigine. Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na+ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al.
    Lamotrigine-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N
  • HY-N0755R
    Rhoifolin (Standard)
    Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines.
    Rhoifolin (Standard)
  • HY-13777AR
    Zoledronic acid monohydrate (Standard)
    		Inducer
    Zoledronic acid (monohydrate) (Standard) is the analytical standard of Zoledronic acid (monohydrate). This product is intended for research and analytical applications. Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
    Zoledronic acid monohydrate (Standard)
  • HY-161197
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
    		Inducer
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH 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-C2-O-C2-OH 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-C2-O-C2-OH
  • HY-116071
    Autophagy-IN-3
    		Inhibitor
    Autophagy-IN-3 (Compound 6k) is an autophagy inhibitor. Autophagy-IN-3 promotes metabolic stress in the tumor microenvironment and enhances the effects of cytostatics in combined treatments.
    Autophagy-IN-3
  • HY-12515AS2
    Nicardipine-d4 hydrochloride
    		Inducer
    Nicardipine-d4 hydrochloride is deuterated labeled Nicardipine hydrochloride (HY-12515A). 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-d<sub>4</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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