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-156165
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
    		Inducer
    Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
  • HY-N0087R
    Gambogic Acid (Standard)
    		Inducer
    Gambogic Acid (Standard) is the analytical standard of Gambogic Acid. This product is intended for research and analytical applications. Gambogic Acid (Beta-Guttiferrin) is derived from the gamboges resin of the tree Garcinia hanburyi. Gambogic Acid (Beta-Guttiferrin) inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50s of 1.47 μM, 1.21 μM, 2.02 μM, 0.66 μM, 1.06 μM and 0.79 μM.
    Gambogic Acid (Standard)
  • HY-138849
    Thalidomide-NH-amido-C2-NH2
    		Inducer
    Thalidomide-NH-amido-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-C2-NH2
  • HY-N3000A
    6-Methoxydihydrosanguinarine hydrochloride
    		Inducer
    6-Methoxydihydrosanguinarine hydrochloride is an alkaloid with activity across multiple cancer cell types. 6-Methoxydihydrosanguinarine hydrochloride activates IRE1/JNK signaling, blocks Akt/mTOR and PI3K/AKT/mTOR pathways, reduces expression of Cdc25C, CyclinB1, Cdc2, YAP/TAZ, Survivin, GPX4, and EGFR, upregulates IRE1 and DR5, and activates JNK and caspases. 6-Methoxydihydrosanguinarine hydrochloride induces apoptosis, G2/M phase arrest, DNA damage, ROS generation, lipid peroxidation, ferroptosis, autophagy, and suppresses cancer cell growth. 6-Methoxydihydrosanguinarine hydrochloride disruptes the biofilm formation of Candida albicans (C. albicans). 6-Methoxydihydrosanguinarine hydrochloride can be used for the research of non-small cell lung cancer, hepatocellular carcinoma, melanoma, colon carcinoma, ovarian cancer and breast cancer.
    6-Methoxydihydrosanguinarine hydrochloride
  • HY-B1000S
    Selenomethionine-76Se
    Selenomethionine-76Se (Seleno-DL-methionine-76Se) is the 76Se- labeled Selenomethionine (HY-B1000). Selenomethionine is a naturally occurring amino acid containing selenium that has oral activity and is a common natural food source. Selenomethionine has antitumor activity.
    Selenomethionine-<sup>76</sup>Se
  • HY-178029
    RSK2/TOP2-IN-1
    		Inducer
    RSK2/TOP2-IN-1 is a RSK2/TOP2 dual inhibitor. RSK2/TOP2-IN-1 targets key tumor progression enzymes including ribosomal S6 kinase 2 and topoisomerases IIα/IIβ. RSK2/TOP2-IN-1 shows selectivity index > 2 against all squamous cell carcinoma (SCC) cell lines. RSK2/TOP2-IN-1 can induce cell apoptosis, autophagy and ROS production. RSK2/TOP2-IN-1 can be used for the research of cancer, such as squamous cell carcinoma.
    RSK2/TOP2-IN-1
  • HY-N1462R
    Atractyloside potassium salt (Standard)
    		Activator
    Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity.
    Atractyloside potassium salt (Standard)
  • HY-10212A
    BIIB021 mesylate
    		Inducer
    BIIB021 (CNF2024) mesylate is the mesylate of BIIB021 (HY-10212). BIIB021 is an orally active Hsp90 inhibitor. BIIB021 inhibits the proliferation of chronic myeloid leukemia (CML) cells, with IC50 values of K562, K562/G, 32Dp210, and 32Dp210-T315I cells are 513.99, 603.53, 110.08, and 148.07 nM, respectively. BIIB021 degrades BCR-ABL protein and inhibits the β-catenin/c-Myc pathway. BIIB021 can also induce autophagy in CML cells. BIIB021 can be used for the research of CML.
    BIIB021 mesylate
  • HY-N2117R
    Isoginkgetin (Standard)
    		Activator
    Isoginkgetin (Standard) is the analytical standard of Isoginkgetin. This product is intended for research and analytical applications. Isoginkgetin is a pre-mRNA splicing inhibitor inhibitor. Isoginkgetin also inhibits activities of both Akt, NF-κB and MMP-9. Isoginkgetin inhibits the activity of the 20S proteasome, induces apoptosis and activates autophagy.
    Isoginkgetin (Standard)
  • HY-B0233S2
    Isradipine-d7
    		Inducer
    Isradipine-d7 is deuterated labeled Isradipine (HY-B0233). Isradipine (PN 200-110) is an orally active L-type calcium channel blocker. Isradipine, as a powerful peripheral vasodilator, is a dihydropyridine calcium antagonist with selective actions on the heart as well as the peripheral circulation. Isradipine is a potentially viable neuroprotective agent for Parkinson's disease.
    Isradipine-d<sub>7</sub>
  • HY-10999S2
    Trametinib-13C,d3
    		Inducer
    Trametinib-13C,d3 is the 13C- and deuterium labeled Trametinib. Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.
    Trametinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-168206
    Autophagy-IN-6
    		Inhibitor
    Autophagy-IN-6 (compound 1u) is a lysosomotropic autophagy inhibitor and can induces LC3-II protein accumulation. Autophagy-IN-6 shows anti-proliferative activity.
    Autophagy-IN-6
  • HY-14266S
    Dapivirine-d11
    		Inducer
    Dapivirine-d11 is the deuterium labeled Dapivirine. Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations.
    Dapivirine-d<sub>11</sub>
  • HY-12033S1
    2-Methoxyestradiol-13C6
    		Inducer
    2-Methoxyestradiol-13C6 is the 13C-labeled 2-Methoxyestradiol. 2-Methoxyestradiol (2-ME2), an orally active endogenous metabolite of 17β-estradiol (E2), is an apoptosis inducer and an angiogenesis inhibitor with potent antineoplastic activity. 2-Methoxyestradiol also destablize microtubules. 2-Methoxyestradio, also a potent superoxide dismutase (SOD) inhibitor and a ROS-generating agent, induces autophagy in the transformed cell line HEK293 and the cancer cell lines U87 and HeLa.
    2-Methoxyestradiol-<sup>13</sup>C<sub>6</sub>
  • HY-N0155R
    Nobiletin (Standard)
    		Inducer
    Nobiletin (Standard) is the analytical standard of Nobiletin. This product is intended for research and analytical applications. Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
    Nobiletin (Standard)
  • HY-P10110
    retro-inverso TAT-Beclin 1 (D-amino acid)
    		Inducer
    retro-inverso TAT-Beclin 1 D-amino acid is has higher activity and resistance to proteolytic degradation in vivo compared to L-amino acids peptide. TAT-Beclin 1 can induce autophagy in peripheral tissues in adult mice as well as in the central nervous system of neonatal mice.
    retro-inverso TAT-Beclin 1 (D-amino acid)
  • HY-10159S1
    Nilotinib-13C,d3
    		Inducer
    Nilotinib-13C,d3 is a deuterated labeled Nilotinib. Nilotinib is an orally available Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity.
    Nilotinib-<sup>13</sup>C,d<sub>3</sub>
  • HY-178349
    P-gp inhibitor 30
    		Inducer
    P-gp inhibitor 30 is a potent P-gp inhibitor that reverses multidrug resistance in breast cancer by sensitizing resistant cells to Doxorubicin (ADM) (HY-15142). P-gp inhibitor 30 promotes apoptosis, induces autophagy, and suppresses proliferation, migration, and invasion of drug-resistant breast cancer cells when combined with ADM. P-gp inhibitor 30 inhibits breast tumor growth both in vitro and in vivo. P-gp inhibitor 30 can be used for drug-resistant breast cancer research.
    P-gp inhibitor 30
  • HY-139547
    Thalidomide-5,6-Cl
    		Inducer
    Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5,6-Cl
  • HY-10181BR
    Dasatinib monohydrate (Standard)
    		Inducer
    Dasatinib (monohydrate) (Standard) is the analytical standard of Dasatinib (monohydrate). This product is intended for research and analytical applications. Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
    Dasatinib monohydrate (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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