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-B0102SA
    Fluoxetine-d6 oxalate
    		Inducer
    Fluoxetine-d6 oxalate (LY-110140-d6 oxalate) is the deuterium labeled Fluoxetine oxalate. Fluoxetine oxalate is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
    Fluoxetine-d<sub>6<sub> oxalate
  • HY-183730
    4E1RCat 17d
    		Inhibitor
    4E1RCat 17d is a derivative of the ATG5 inhibitor lead compound T1742 (HY-183807). 4E1RCat 17d shows no activity against the interactions of ATG5-ATG16L1 and ATG5-TECAIR. 4E1RCat 17d induces Autophagy inhibition.
    4E1RCat 17d
  • HY-N10611
    Elsinochrome A
    		Inducer
    Elsinochrome A is a perylene quinone photosensitizer, and can generate reactive oxygen species (ROS) to induce apoptosis and autophagy under light excitation. Elsinochrome A also shows antifungal activity against C. albicans biofilm through photodynamic antimicrobial chemotherapy (PACT). Elsinochrome A can be used for research of photodynamic therapy (PDT) (Ex: 460 nm).
    Elsinochrome A
  • HY-168892
    LC3B recruiter 2
    		98.11%
    LC3B recruiter 2 (34R) is an LC3B recruiter and a component of the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), which directly binds to LC3B. LC3B recruiter 2 binds to CDK9 inhibitor SNS-032 (HY-10008) through a linker, forming an ATTEC that targets the degradation of the CDK9 and Cyclin T1 complex (with inhibitory effects on both). Therefore, LC3B recruiter 2 exerts activity through the LC3B-dependent autophagy-lysosome pathway, interfering with the cell cycle of cancer cells, thus exhibiting antitumor activity.
    LC3B recruiter 2
  • HY-123255
    BSc2118
    		Inhibitor
    BSc2118 is a 20S proteasome inhibitor with an IC50 of approximately 50 nM. BSc2118 induces G2/M phase cell cycle arrest and apoptosis in myeloma cells, inhibits cytoprotective autophagy, and suppresses tumor angiogenesis. BSc2118 reduces MMP9 activity, promotes angioneurogenesis, and alleviates recombinant tissue-type plasminogen activator-induced cerebral toxicity. BSc2118 is applicable to studies related to cerebral ischemia and multiple myeloma.
    BSc2118
  • HY-A0005R
    Clofarabine (Standard)
    		Inducer
    Clofarabine (Standard) is the analytical standard of Clofarabine. This product is intended for research and analytical applications. Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit.
    Clofarabine (Standard)
  • HY-W765245
    Rapamycin-13C,d3-1
    Rapamycin-13C,d3-1 (Sirolimus-13C,d3-1) is the deuterium labeled and 13C-labeled Rapamycin (HY-10219). Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.
    Rapamycin-<sup>13</sup>C,d<sub>3</sub>-1
  • HY-B0338AR
    Rimantadine hydrochloride (Standard)
    		Inducer
    Rimantadine (hydrochloride) (Standard) is the analytical standard of Rimantadine (hydrochloride). This product is intended for research and analytical applications. Rimantadine is an orally active inhibitor for M2 protein, that blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity.
    Rimantadine hydrochloride (Standard)
  • HY-N0752R
    Scutellarein (Standard)
    		Inducer
    Scutellarein (Standard) is the analytical standard of Scutellarein. This product is intended for research and analytical applications. Scutellarein is a natural flavonoid compound with anti-inflammatory effects.
    Scutellarein (Standard)
  • HY-161201
    Thalidomide-piperazine-pyrimidine-piperazine-C-boc
    		Inducer
    Thalidomide-piperazine-pyrimidine-piperazine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-pyrimidine-piperazine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-pyrimidine-piperazine-C-boc
  • HY-N3855
    Erythrabyssin II
    		Inhibitor
    Erythrabyssin II (EL-19) is a potent late-stage autophagy inhibitor that blocks the fusion of autophagosome and lysosome. Erythrabyssin II leads to the accumulation of autophagic substrates and does not impair lysosomal pH or lysosomal enzyme activity. Erythrabyssin II suppresses ovarian cancer organoid activity and induces apoptosis. Erythrabyssin II can be used for the study of ovarian cancer.
    Erythrabyssin II
  • HY-14648S1
    Dexamethasone-d5-1
    		Inducer
    Dexamethasone-d5-1 is deuterium labeled Dexamethasone. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
    Dexamethasone-d<sub>5</sub>-1
  • HY-183273
    BRD4/AKT-IN-1
    		Inducer
    BRD4/AKT-IN-1 is a BRD4/AKT inhibitor with BRD4 IC50 66.12 nM and AKT1 IC50 143.81 nM. BRD4/AKT-IN-1 blocks BRD4-mediated c-Myc transcriptional regulation, modulates AKT1 signaling, decouples AKT phosphorylation from pro-survival effectors. BRD4/AKT-IN-1 induces G0/G1 cell cycle arrest via downregulated phosphorylated RB, cyclin E1, CDK2. BRD4/AKT-IN-1 elevates LC3B levels to promote autophagy. BRD4/AKT-IN-1 promotes apoptosis in cancer cells. BRD4/AKT-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.
    BRD4/AKT-IN-1
  • HY-139543
    Thalidomide-5-PEG2-Cl
    		Inducer
    Thalidomide-5-PEG2-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-PEG2-Cl can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-PEG2-Cl
  • HY-10882R
    Clotrimazole (Standard)
    		Inhibitor
    Clotrimazole (Standard) is the analytical standard of Clotrimazole. This product is intended for research and analytical applications. Clotrimazole is an imidazole derivative, an antifungal compound and is a CYP (cytochrome P450) inhibitor. Clotrimazole has antibacterial activity.
    Clotrimazole (Standard)
  • HY-172255
    PI4KIII beta inhibitor 4
    		Inducer
    PI4KIII beta inhibitor 4 (Compound 16) is a selective PI4KIIIβ inhibitor with an IC50 of 0.005 μM. PI4KIIIβ inhibitor 4 induces tumor cell apoptosis, cell cycle arrest, and autophagy by inhibiting the PI3K/AKT pathway. PI4KIIIβ inhibitor 4 can be used in the study of cancer.
    PI4KIII beta inhibitor 4
  • HY-B0180S1
    Imiquimod-d9
    		Inducer
    Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19.
    Imiquimod-d<sub>9</sub>
  • HY-138852A
    Thalidomide-NH-amido-C6-NH2 (hydrochloride)
    		Inducer
    Thalidomide-NH-amido-C6-NH2 hydrochloride 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-C6-NH2 (hydrochloride)
  • HY-B0450S
    Ciclopirox-d11
    		Inducer
    Ciclopirox-d11 is the deuterium labeled Ciclopirox. Ciclopirox (HOE296b) is a synthetic antifungal agent that can be used for superficial mycoses reseaech. Ciclopirox olamine has a very broad spectrum of activity and inhibits dermatophytes, yeasts, molds, and many Gram-positive and Gram-negative species pathogenic.
    Ciclopirox-d<sub>11</sub>
  • HY-12009R
    Pazopanib Hydrochloride (Standard)
    		Inducer
    Pazopanib (Hydrochloride) (Standard) is the analytical standard of Pazopanib (Hydrochloride). This product is intended for research and analytical applications. Pazopanib Hydrochloride (GW786034 Hydrochloride) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with an IC50 of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
    Pazopanib Hydrochloride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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