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-W758421
    Diquat-d8(dibromide)
    Diquat-d8 dibromide is a deuterium labeled Diquat dibromide (HY-122984). Diquat dibromide is a comprehensive herbicide. Diquat dibromide increases the production of ROS and triggers mitochondrial Autophagy. Diquat dibromide generates free radicals such as superoxide anions through redox cycles, which induce oxidative stress. Diquat dibromide is cytotoxic, reproductive, and neurotoxic. Diquat dibromide is used in cotton, soybean, and other crops to combat noxious weeds.
    Diquat-d<sub>8</sub>(dibromide)
  • HY-13955S1
    Telmisartan-d4
    		Inducer
    Telmisartan-d4 is the deuterium labeled Telmisartan. Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
    Telmisartan-d<sub>4</sub>
  • HY-17504C
    (3R,5R)-Rosuvastatin
    		Activator
    (3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
    (3R,5R)-Rosuvastatin
  • HY-117985BS
    Evogliptin-d9 tartrate
    		Inducer
    Evogliptin-d9 tartrate (DA-1229-d9 tartrate) is the deuterium labeled Evogliptin tartrate (HY-117985B). Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation.
    Evogliptin-d<sub>9</sub> tartrate
  • HY-10820S
    Pemetrexed-d5
    Pemetrexed-d5 is the deuterium labeled Pemetrexed. Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively.
    Pemetrexed-d<sub>5</sub>
  • HY-125535
    OSU-53
    		Inducer
    OSU-53 is an orally active AMPK activator (EC50: 0.3 μM) and a direct mTOR inhibitor. OSU-53 induces autophagy and increases conversion of LC3 I to LC3 II. OSU-53 also modulates energy homeostasis by suppressing fatty acid biosynthesis and shifting the metabolism to oxidation by up-regulating the expression of PGC1α and NRF-1. OSU-53 has antitumor activity in various tumor models, such as breast cancer and thyroid cancer.
    OSU-53
  • HY-147520
    FAK-IN-5
    		Inducer
    FAK-IN-5 (Compound 8l) is a FAK signaling inhibitor. FAK-IN-5 induces cell apoptosis and autophagy.
    FAK-IN-5
  • HY-12956S1
    Dinoprost-d9
    		Inducer
    Dinoprost-d9 is the deuterium labeled Dinoprost. Dinoprost (Prostaglandin F2α) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost plays a key role in the onset and progression of labour.
    Dinoprost-d<sub>9</sub>
  • HY-50878AS
    Crizotinib-d9 hydrochloride
    		Inducer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.
    Crizotinib-d<sub>9</sub> hydrochloride
  • HY-D2971
    NCIC-VIS
    NCIC-VIS is a lysosome-targeted, viscosity-sensitive two-photon near-infrared fluorescent probe. NCIC-VIS has a rigid structure that can restrict molecular torsion, thereby increasing the fluorescence quantum yield and two-photon absorption cross-section. NCIC-VIS enables real-time imaging of the autophagy process in cells.
    NCIC-VIS
  • HY-N0400R
    Wogonin (Standard)
    		Inducer
    Wogonin (Standard) is the analytical standard of Wogonin. This product is intended for research and analytical applications. Wogonin is a naturally occurring mono-flavonoid, can inhibit the activity of CDK8 and Wnt, and exhibits anti-inflammatory and anti-tumor effects.
    Wogonin (Standard)
  • HY-D3211
    HJTA
    		Inducer
    HJTA is a selective, pH/GSH dual-responsive Fluorescent probe and anticancer agent. HJTA selectively undergoes an enzymatic reaction with GSTπ. HJTA induces Apoptosis and Autophagy by regulating the expression of apoptotic and autophagic proteins. HJTA exhibits pH- and GSH-dual-responsive fluorescence in tumor cells. HJTA selectively illuminates tumor tissues, enabling precise in situ visualization of colon tumors. HJTA exerts anticancer effects against colon cancer. HJTA can be used for colon cancer research.
    HJTA
  • HY-181724
    501A054
    		Activator
    501A054 is an autophagy activator. 501A054 induces autophagy-dependent cell death via autophagy activation. 501A054 can be used in studies on autophagy regulation such as cervical cancer.
    501A054
  • HY-163236
    Thalidomide-piperidine-O-azetidine-acetic acid
    		Inducer
    Thalidomide-piperidine-O-azetidine-acetic acid is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-O-azetidine-acetic acid can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperidine-O-azetidine-acetic acid
  • HY-181062
    VWK147
    		Inducer
    VWK147 is a second-generation HSP90 C-terminal domain (CTD) inhibitor. VWK147 targets the CTD dimerization interface, prevents HSP90 CTD dimerization, disrupts co-chaperone PPID binding to HSP90 CTD, and inhibits HSP90 chaperone function dependent on dimerization. VWK147 reduces protein levels of HSP90 client proteins ULK1, RIPK1, and CDK4 without inducing a heat shock response. VWK147 induces cell death, including apoptosis, in Cisplatin (HY-17394)-sensitive and -resistant urothelial carcinoma cells. VWK147 induces LC3-II accumulation, inhibits autophagosome-lysosome fusion to block canonical autophagy, and induces non-canonical LC3 lipidation independent of ULK1 and PIK3C3 complexes. VWK147 can be used for the research of urothelial carcinoma.
    VWK147
  • HY-144782
    HDAC10-IN-2
    		Inducer
    HDAC10-IN-2 (compound 10c) is a potent and highly selective HDAC10 inhibitor, with an IC50 of 20 nM. HDAC10-IN-2 modulates autophagy in aggressive FLT3-ITD positive acute myeloid leukemia cells.
    HDAC10-IN-2
  • HY-B0532AS
    Trifluoperazine-d3 dihydrochloride
    		Inhibitor
    Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis.
    Trifluoperazine-d<sub>3</sub> dihydrochloride
  • HY-159007
    BD-AcAc2
    		Inducer
    BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity.
    BD-AcAc2
  • HY-13677S3
    6-Mercaptopurine-13C,15N2
    		Inhibitor
    6-Mercaptopurine-13C,15N2 (Mercaptopurine-13C,15N2) is the 13C- and 15N-labeled 6-Mercaptopurine (HY-13677). 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
    6-Mercaptopurine-<sup>13</sup>C,<sup>15</sup>N<sub>2</sub>
  • HY-12008S1
    Erlotinib-13C6 hydrochloride
    Erlotinib-13C6 hydrochloride is the 13C labeled Erlotinib Hydrochloride. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM. Erlotinib-13C6 hydrochloride is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    Erlotinib-<sup>13</sup>C<sub>6</sub> hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
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