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-14664DS
    (3S,5R)-Fluvastatin-d6
    		Inducer
    (3S,5R)-Fluvastatin-d6 is the deuterium labeled (3S,5R)-Fluvastatin sodium. Fluvastatin is a first fully synthetic, competitive HMG-CoA reductase inhibitor with an IC50 of 8 nM. Fluvastatin protects vascular smooth muscle cells against oxidative stress through the Nrf2-dependent antioxidant pathway[1].
    (3S,5R)-Fluvastatin-d<sub>6</sub>
  • HY-14649S5
    Retinoic acid-d3
    Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid-d<sub>3</sub>
  • HY-10260S1
    Vandetanib-d4
    		Inducer
    Vandetanib-d4 is the deuterium labeled Vandetanib. Vandetanib (ZD6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)[1][2].
    Vandetanib-d<sub>4</sub>
  • HY-N0716AR
    Berberine (hemisulfate) (Standard)
    		Inducer
    Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine (hemisulfate) (Standard)
  • HY-B0450S1
    Ciclopirox-d11 sodium
    		Inducer
    Ciclopirox-d11 (sodium) is 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[1].
    Ciclopirox-d<sub>11</sub> sodium
  • HY-B0309S1
    Felodipine-d5
    		Inducer
    Felodipine-d5 is deuterium labeled Felodipine. Felodipine, a dihydropyridine, is a potent, vasoselective calcium channel antagonist. Felodipine lowers blood pressure (BP) by selective action on vascular smooth muscle, especially in the resistance vessels. Felodipine, an anti-hypertensive agent, induces autophagy. Felodipine can cross the blood-brain barrier[1][2][3].
    Felodipine-d<sub>5</sub>
  • HY-W700643
    Di-N-desethyl amiodarone hydrochloride
    		Inducer
    Di-N-desethyl Amiodarone hydrochloride is a metabolite of Amiodarone (HY-14187). Di-N-desethyl Amiodarone hydrochloride is a strong inhibitor of the respiratory chain.
    Di-N-desethyl amiodarone hydrochloride
  • HY-169022
    4-FPBUA
    		Inducer
    4-FPBUA is a semisynthetic analog of usnic acid (HY-W015883) that can enhance cellular blood-brain barrier (BBB) function and increase the transport of Amyloid β (Aβ) across monolayer cells. 4-FPBUA is also an inhibitor of mTOR, capable of enhancing cellular Autophagy, thereby reversing BBB disruption in vivo and being utilized in research for Alzheimer's disease.
    4-FPBUA
  • HY-172201
    NF-κB-IN-19
    		Inducer
    NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. NF-κB-IN-19 effectively induces DNA damage, promotes the generation of ROS, and induces autophagy and apoptosis through the NF-κB signaling pathway in tumor cells. In addition, NF-κB-IN-19 can inhibit the levels of VEGF and HIF-1α, and exert antiproliferative activity in tumor cells through the PI3K/AKT and STAT-3 pathways. NF-κB-IN-19 can effectively overcome cisplatin resistance and has anti-tumor activity.
    NF-κB-IN-19
  • HY-124896
    Bonannione A
    		Inducer
    Bonannione A (6-Geranylnaringenin; Mimulone), a prenylflavonoid, is an orally active and potent protein tyrosine phosphatase 1B (PTP1B) inhibitor with an IC50 of 14 µM. Bonannione A triggers caspase-dependent apoptosis. Bonannione A induces autophagy through p53-mediated AMPK/mTOR pathway. Bonannione A shows anti-inflammatory, antiradical and anti-cancer activity.
    Bonannione A
  • HY-42771
    Thalidomide-4-O-CH2-COO(t-Bu)
    		Inducer
    Thalidomide-4-O-CH2-COO(t-Bu) is t-Bu modified Thalidomide (HY-14658), which is the final step intermediate in the synthesis of Thalidomide-4-OH (HY-123096). Thalidomide-4-O-CH2-COO(t-Bu) acts as a Cereblon ligand to recruit CRBN proteins. The t-Bu protecting group at the end of Thalidomide-4-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based designed PROTAC molecules.
    Thalidomide-4-O-CH2-COO(t-Bu)
  • HY-161205
    Thalidomide-PIP-(R)C-pyrrolidine-boc
    		Inducer
    Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-PIP-(R)C-pyrrolidine-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-PIP-(R)C-pyrrolidine-boc
  • HY-161184
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
    		Inducer
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-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.
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
  • HY-162310
    Anticancer agent 193
    		Inducer
    Anticancer agent 193 (compound D3-3) is an inducer of ferritinophagy, eventually triggering ferroptosis. Anticancer agent 193 induces the production of lipid ROS, and significantly promoted colorectal cancer cells to release the ferrous ion in an autophagy-dependent manner.
    Anticancer agent 193
  • HY-N0156S
    Oleanolic acid-d3
    Oleanolic acid-d3 is the deuterium labeled Oleanolic Acid[1]. Oleanolic acid (Caryophyllin) is a natural compound from plants with anti-tumor activities[2].
    Oleanolic acid-d<sub>3</sub>
  • HY-N10408
    Tripchlorolide
    		Inducer
    Tripchlorolide is a neuroprotective agent that can be found in Tripterygium wilfordii. Tripchlorolide prevents tumor growth by inducing apoptosis and autophagy. Tripchlorolide improves cognitive deficits in Alzheimer's disease.
    Tripchlorolide
  • HY-169824
    TRPML modulator 1
    		Inducer
    TRPML modulator 1 (compound A12) is a TRPML modulator that promotes autophagy. TRPML modulator 1 AC50 in the TFEB test is less than 2 mM.
    TRPML modulator 1
  • HY-B0172S1
    Lithocholic acid-d5
    		Inducer
    Lithocholic acid-d5 is deuterium labeled Lithocholic acid.
    Lithocholic acid-d<sub>5</sub>
  • HY-W016409R
    Ethyl 3,4-dihydroxybenzoate (Standard)
    		Inducer
    Ethyl 3,4-dihydroxybenzoate (Standard) (Protocatechuic acid ethyl ester (Standard)) is the analytical standard of Ethyl 3,4-dihydroxybenzoate (HY-W016409). This product is intended for research and analytical applications. Ethyl 3,4-dihydroxybenzoate (Protocatechuic acid ethyl ester) is an orally effective, blood-brain barrier-permeable, competitive prolyl hydroxylase (PHD) inhibitor that inhibits the hydroxylation modification of hypoxia-inducible factor (HIF) by PHD. Ethyl 3,4-dihydroxybenzoate stabilizes HIF-1α by inhibiting PHD, activates downstream pathways to induce autophagy and apoptosis of tumor cells, and regulates inflammatory responses, inhibits the NF-κB pathway, improves vascular permeability, and promotes osteoblast differentiation. Ethyl 3,4-dihydroxybenzoate has anti-tumor, anti-hypoxic injury, and bone metabolism regulation effects. It can also be used in the research of cardiovascular protection (such as reducing myocardial ischemic damage), bone tissue engineering (promoting osteogenesis/inhibiting osteoclast differentiation), and prevention and treatment of high-altitude cerebral edema.
    Ethyl 3,4-dihydroxybenzoate (Standard)
  • HY-121726
    3HOI-BA-01
    		Inducer
    3HOI-BA-01 is amTORinhibitor.3HOI-BA-01reduces infarct size and inducedautophagyin a murine myocardial ischemia/reperfusion injury model.
    3HOI-BA-01
Cat. No. Product Name / Synonyms Application Reactivity
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