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-141012
    Thalidomide-O-PEG4-NHS ester
    		Inducer 98.76%
    Thalidomide-O-PEG4-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.
    Thalidomide-O-PEG4-NHS ester
  • HY-161724
    TFEB activator 2
    		Modulator 98.84%
    TFEB activator 2 is an orally active compound that can cross the blood-brain barrier. TFEB activator 2 can bind to the dopamine transporter (DAT). TFEB activator 2 promotes TFEB nuclear translocation and lysosome biogenesis by targeting the DAT-CDK9-TFEB pathway. TFEB activator 2 has neuroprotective activity and can be used in the research of Alzheimer's disease and other diseases.
    TFEB activator 2
  • HY-P4808A
    PHF6 TFA
    		Activator 99.45%
    PHF6 (VQIVYK) TFA is a self-assembly sequence capable of initiating the full-length tau protein aggregation. PHF6 TFA is mapped to the third microtubule-binding repeat region of the tau protein.
    PHF6 TFA
  • HY-15371R
    Forskolin (Standard)
    		Inducer
    Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
    Forskolin (Standard)
  • HY-N3980
    Guaiol
    		99.67%
    Guaiol is a sesquiterpenoid alcohol with oral activity found in various traditional Chinese medicines, exhibiting biological activities such as anti-proliferative, autophagy-promoting, insecticidal, anti-anxiety, anti-inflammatory, diuretic, and blood pressure-lowering effects. Guaiol induces apoptosis in non-small cell lung cancer cells by regulating the stability of RAD51 through autophagy modulation. Guaiol can also act directly on parasites, inhibiting their growth by affecting the kinetoplast, mitochondrial matrix and plasma membrane of the promastigotes. Guaiol kills amastigotes at an IC50 of 0.01 µg/mL. Guaiol can be used in research related to cancer, infections, cardiovascular diseases, and inflammatory conditions[4]
    Guaiol
  • HY-N6002
    3'-Hydroxypterostilbene
    		Inducer 99.89%
    3'-Hydroxypterostilbene is a Pterostilbene (HY-N0828) analogue. 3'-Hydroxypterostilbene inhibits the growth of COLO 205, HCT-116 and HT-29 cells with IC50s of 9.0, 40.2 and 70.9 μM, respectively. 3'-Hydroxypterostilbene significantly down-regulates PI3K/Akt and MAPKs signaling pathways and effectively inhibits the growth of human colon cancer cells by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene can be used for the research of cancer.
    3'-Hydroxypterostilbene
  • HY-17508S
    Clarithromycin-13C,d3
    		99.9%
    Clarithromycin-13C,d3 is the deuterium and 13C labeled Clarithromycin.
    Clarithromycin-<sup>13</sup>C,d<sub>3</sub>
  • HY-119137
    AMDE-1
    		Inducer 99.91%
    AMDE-1 is a potent autophagy inducer. AMDE-1 induces autophagy by the AMPK-mTORC1-ULK1 pathway and at the same time inhibited autophagy-mediated degradation by causing lysosome dysfunction. AMDE-1 can be used in research of cancer.
    AMDE-1
  • HY-N1201R
    Apigenin (Standard)
    		Inducer
    Apigenin (Standard) is the analytical standard of Apigenin. This product is intended for research and analytical applications. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a Ki of 2 μM.
    Apigenin (Standard)
  • HY-101795
    Larixyl acetate
    		99.44%
    Larixyl acetate is a potent and selective TRPC6 inhibitor with IC50 values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.
    Larixyl acetate
  • HY-13756S
    Tacrolimus-13C,d2
    		Inducer 98.36%
    Tacrolimus-13C,d2 is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.
    Tacrolimus-<sup>13</sup>C,d<sub>2</sub>
  • HY-116506
    Bigelovin
    		Inducer 99.92%
    Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation.
    Bigelovin
  • HY-12845
    UNC2400
    		Activator 99.92%
    UNC2400 is a close analog of UNC1999 with >1,000-fold lower potency than UNC1999 as a negative control for cell-based studies.
    UNC2400
  • HY-100746
    STF-62247
    		Inducer 98.69%
    STF-62247 is an autophagy inducer that selectively cytotoxic to VHL-deficient renal cell carcinoma (IC50 of 0.625 μM and 16 μM in RCC4 and RCC4/VHL cells, respectively).
    STF-62247
  • HY-B0338
    Rimantadine
    		Inducer 99.86%
    Rimantadine (1-Rimantadine) is an orally active inhibitor for M2 protein, which blocks the hydrogen ion channel activity, prevents the entry and replication of the virus, and exhibits board-spectrum antiviral activity. Rimantadine significantly inhibits hepatitis A virus (HAV) replication at the post-entry stage in Huh7 cells. Rimantadine enhances autophagy. Rimantadine has a significant protective effect against H3N2 virus in mouse model.
    Rimantadine
  • HY-B0960
    Sulfabenzamide
    		Inducer 99.68%
    Sulfabenzamide (N-Sulfanilylbenzamide) is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
    Sulfabenzamide
  • HY-16682
    AGN 196996
    		99.76%
    AGN 196996 is a potent and selective RARα antagonist with Ki value of 2 nM; little binding affinity for RARβ(Ki=1087 nM) and RARγ(Ki=8523 nM).
    AGN 196996
  • HY-112440
    HZX-02-059
    		Inhibitor 99.40%
    HZX-02-059 is an allosteric inhibitor of PIKFYVE, and a methuosis inducer. HZX-02-059 disrupts the PIKfyve/TFEB axis, suppresses tubulin polymerization, reduces phosphorylated mTOR levels, downregulates p53, PI3K/AKT, c-Myc, and NF-κB pathways. HZX-02-059 induces G2/M cell cycle arrest, apoptosis, and inhibits cancer cell proliferation. HZX-02-059 can be used for the research of lymphoma, double-hit lymphoma, and B-cell acute lymphoblastic leukemia.
    HZX-02-059
  • HY-B0372A
    Bromhexine hydrochloride
    		Inducer 99.93%
    Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
    Bromhexine hydrochloride
  • HY-N0120AR
    Polydatin (Standard)
    		Inducer
    Polydatin (Standard) is the analytical standard of Polydatin. This product is intended for research and analytical applications. Polydatin (Piceid), extracted from the roots of Reynoutria japonica, a widely used traditional Chinese remedies, possesses anti-inflammatory activity in several experimental models. Polydatin (Piceid) inhibits G6PD and induces oxidative and ER stresses.
    Polydatin (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
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