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-170594
    Antitumor agent-192
    		Inducer
    Antitumor agent-192 (Compound 2f) is a β-carboline antitumor agent. Antitumor agent-192 induces autophagy in HCT116 cells via the ATG5/ATG7 pathway. Antitumor agent-192 has an IC50 of less than 5 μM for human tumor cell lines and significantly inhibits tumor development and reduces tumor weight in a mouse colorectal cancer model transplanted with allografts[1].
    Antitumor agent-192
  • HY-150757
    Autophagy-IN-2
    		Inhibitor
    Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research.
    Autophagy-IN-2
  • HY-124132
    Autophagy-IN-4
    		Inhibitor 99.35%
    Autophagy-IN-4 (Compound 34) is an autophagy inhibitor, with an EC50 of 0.5 μM and a LD50 of 27 μM for U2OS cells.
    Autophagy-IN-4
  • HY-B1693A
    Levomepromazine hydrochloride
    		Inducer
    Levomepromazine (Methotrimeprazine) hydrochloride is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine hydrochloride has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine hydrochloride can induce adaptive ER stress and autophagy. In addition, Levomepromazine hydrochloride has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine hydrochloride can be used in the study psychiatric disorders and relieving nausea and vomiting.
    Levomepromazine hydrochloride
  • HY-50898S1
    Lapatinib-d7 dihydrochloride
    		Inducer
    Lapatinib-d7 dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride 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-d<sub>7</sub> dihydrochloride
  • HY-161190
    Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-C2-OH
    		Inducer
    Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-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-piperidine-C-2,6-diazaspiro[3.3]heptane-C2-OH
  • HY-10181G
    Dasatinib (GMP)
    		Inducer
    Dasatinib (BMS-354825) (GMP) is a GMP-grade Dasatinib (HY-10181). GMP-grade small molecules can be used as adjuvant agents in cell therapy. Dasatinib (BMS-354825) is an orally active, ATP-competitive, dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Ki values ​​for Src and Bcr-Abl are 16 pM and 30 pM, respectively. Dasatinib inhibits Bcr-Abl and Src with IC50 values ​​of less than 1.0 nM and 0.5 nM, respectively. Dasatinib also induces apoptosis and autophagy.
    Dasatinib (GMP)
  • HY-111261
    UNBS3157
    		Inducer
    UNBS3157 is a naphthalimide derivative that shows potent anticancer effect. UNBS3157 induces autophagy and senescence in cancer cells. UNBS3157 displays significant antitumor effects in vivo. UNBS3157 can be used for leukemia, mammary adenocarcinoma, non-small cell lung cancer (NSCLC) and pancreatic cancer research.
    UNBS3157
  • HY-149829
    Antitumor agent-97
    		Inhibitor
    Antitumor agent-97 (compound 42) is an anticancer agent. Antitumor agent-97 can effectively inhibit the proliferation and autophagy of MGC 803 cells, and induce apoptosis. Antitumor agent-97 also enhances ROS accumulation in MGC 803 cells. Antitumor agent-97 can be used in cancer research.
    Antitumor agent-97
  • HY-15682R
    TTNPB (Standard)
    TTNPB (Standard) is the analytical standard of TTNPB. This product is intended for research and analytical applications. TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
    TTNPB (Standard)
  • 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)
Cat. No. Product Name / Synonyms Application Reactivity
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