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-170667
    Autophagy activator-1
    		Activator
    Autophagy activator-1 (Compound B2) is an autophagy activator Autophagy. Activator-1 ultimately leads to the activation of autophagy by downregulating key members of the HSP70 family and activating the unfolded protein response.
    Autophagy activator-1
  • HY-17401S
    Ranolazine-d8 dihydrochloride
    		Inducer 99.0%
    Ranolazine-d8 (dihydrochloride) is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina agent that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor.
    Ranolazine-d<sub>8</sub> dihydrochloride
  • HY-103691
    ARN5187
    		Inhibitor
    ARN5187 is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 shows lysosomotropic potency and cytotoxicity. ARN5187 induces apoptosis.
    ARN5187
  • HY-159483
    SelB-1
    		Inducer
    SelB-1 serves as a dual inhibitor for Topoisomerase I/II. SelB-1 possesses anticancer activity and can be utilized in the research of prostate cancer and colon cancer. Furthermore, SelB-1 is also capable of inducing autophagy gene expression and lipid peroxidation, while simultaneously reducing the level of GSH.
    SelB-1
  • HY-P2260A
    Tat-beclin 1 TFA
    		Inducer
    Tat-beclin 1 TFA, a peptide derived from a region of the autophagy protein (beclin 1), is a potent inducer of autophagy and interacts with negative regulator of autophagy, GAPR-1 (GLIPR2). Tat-beclin 1 TFA decreases the accumulation of polyglutamine expansion protein aggregates and the replication of several pathogens (including HIV-1) in vitro, and reduces mortality in mice infected with chikungunya (CHIKV) or West Nile virus (WNV).
    Tat-beclin 1 TFA
  • HY-181805
    HDAC6-IN-76
    		Inducer
    HDAC6-IN-76 (Compound G25) is a selective HDAC6 inhibitor with an IC50 of 12 nM. HDAC6-IN-76 induces Autophagy in a p53-dependent manner. HDAC6-IN-76 induces Apoptosis in a p53-dependent manner. HDAC6-IN-76 exhibits anticancer activity against hematologic malignancies, including acute myeloid leukemia.
    HDAC6-IN-76
  • HY-114118C
    Semaglutide sodium
    		Activator
    Semaglutide sodium is a long-acting, selective, competitive GLP-1R agonist that can penetrate the blood-brain barrier. After activating GLP-1R, Semaglutide sodium promotes insulin secretion, inhibits gastric emptying and appetite, and at the same time enhances autophagy, inhibits oxidative stress and apoptosis. Semaglutide sodium also regulates mitochondrial function and lipid metabolism (such as reducing de novo lipogenesis in the liver). Semaglutide sodium has activities such as lowering blood sugar, reducing weight, neuroprotection (such as improving motor function in Parkinson's disease models, reducing α-synuclein aggregation) and improving hepatic steatosis. Semaglutide sodium can be used for the study of neurodegenerative diseases and liver diseases such as type 2 diabetes, obesity, Parkinson's disease, metabolic associated fatty liver disease (MASLD), and cancer.
    Semaglutide sodium
  • HY-112774
    ICSN3250
    		Inducer
    ICSN3250 is a halitulin analogue and specific mTORC1 inhibitor. ICSN3250 directly binds to mTOR's FRB domain and displaces phosphatidic acid (PA), reversing mTORC1 activation. ICSN3250 shows high cytotoxicity in cancer cells (nanomolar concentration) through a caspase-independent cell death mechanism. ICSN3250 specifically inhibits the mTORC1 pathway, inducing autophagy and G0-G1 cell-cycle arrest in cancer cells. ICSN3250 can be used for the study of cancer.
    ICSN3250
  • HY-157749
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
    		Inducer
    Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET.
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
  • HY-N1435R
    Oroxin B (Standard)
    Oroxin B (Standard) is the analytical standard of Oroxin B. This product is intended for research and analytical applications. Oroxin B (OB) is a flavonoid isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent. Oroxin B (OB) possesses obvious inhibitory effect and induces early apoptosis rather than late apoptosis on liver cancer cells through upregulation of PTEN, down regulation of COX-2, VEGF, PI3K, and p-AKT. Oroxin B (OB) selectively induces tumor-suppressive ER stress in malignant lymphoma cells.
    Oroxin B (Standard)
  • HY-N6772R
    Cytochalasin E (Standard)
    		Inhibitor
    Antazoline (phosphate) (Standard) is the analytical standard of Antazoline (phosphate). This product is intended for research and analytical applications. Antazoline phosphate is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect.
    Cytochalasin E (Standard)
  • HY-B2098A
    Lucanthone hydrochloride
    		Inhibitor
    Lucanthone hydrochloride is an endonuclease inhibitor of Apurinic endonuclease-1 (APE-1).
    Lucanthone hydrochloride
  • HY-141014
    Thalidomide-O-PEG4-Boc
    		Inducer
    Thalidomide-O-PEG4-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.
    Thalidomide-O-PEG4-Boc
  • HY-174157
    AR493
    		Activator
    AR493 is an autophagy activator acting on AMPK (adenosine monophosphate-activated protein kinase). AR493 regulates pathways related to cellular energy sensing and increases autophagy levels. AR493 is promising for research of aging-associated diseases (such as diabetes, neurodegenerative diseases) and autophagy regulation.
    AR493
  • HY-168507
    SG31
    		Inducer
    SG31 is a potent autophagy activator via the AMPK/ULK1-dependent pathway.
    SG31
  • HY-B0492S1
    Paroxetine-d4 hydrochloride
    		Inducer 99.16%
    Paroxetine-d4 (hydrochloride) is deuterium labeled Paroxetine (hydrochloride). Paroxetine hydrochloride is a potent selective serotonin-reuptake inhibitor, commonly prescribed as an and has GRK2 inhibitory ability with IC50 of 14?μM. Paroxetine hydrochloride can be used for the research of depressive disorder.
    Paroxetine-d<sub>4</sub> hydrochloride
  • HY-180188
    F1-ispinesib
    		Inducer
    F1-ispinesib is a heterobifunctional F1-autophagy degrader, composed of an RNA-binding fragment (F1) and the LC3B ligand Ispinesib (HY-50759). F1-ispinesib induces degradation of COL15A1 mRNA via an LC3B-dependent macroautophagy mechanism. F1-ispinesib inhibits cell proliferation and enhances migration of human aortic smooth muscle cells.
    F1-ispinesib
  • HY-13287A
    SGI-1776
    		Inducer
    SGI-1776 is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, Pim-2 and Pim-3, respectively.
    SGI-1776
  • HY-139207A
    Glucosamine sulfate sodium chloride
    Glucosamine sulfate sodium chloride is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids, is used as a dietary supplement. Glucosamine sulfate sodium chloride also is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, which when administered exogenously, exerts pharmacological effects on osteoarthritic cartilage and chondrocytes.
    Glucosamine sulfate sodium chloride
  • HY-138851A
    Thalidomide-NH-amido-C5-NH2 hydrochloride
    		Inducer
    Thalidomide-NH-amido-C5-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-C5-NH2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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