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-Y1269S
    Ammonium chloride-15N
    		Inhibitor 98.0%
    Ammonium chloride-15N is the 15N labeled Ammonium chloride (HY-Y1269). Ammonium chloride, as a heteropolar compound with pH value regulation, can cause intracellular alkalization and metabolic acidosis thus effecting enzymatic activity and influencing the process of biological system. Ammonium chloride is an autophagy inhibitor. Ammonium chloride is also a lysosome inhibitor.
    Ammonium chloride-<sup>15</sup>N
  • HY-15465A
    KN-93 hydrochloride
    		99.64%
    KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
    KN-93 hydrochloride
  • HY-10130
    Veliparib dihydrochloride
    		Inducer 99.98%
    Veliparib (dihydrochloride) is a potent inhibitor of PARP1 and PARP2 with Kis of 5.2 nM and 2.9 nM in cell-free assays, respectively.
    Veliparib dihydrochloride
  • HY-10291
    Tarenflurbil
    		99.95%
    Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.
    Tarenflurbil
  • HY-N6779
    Patulin
    		Inducer 99.70%
    Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, causes chromosome breakage, mutation, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
    Patulin
  • HY-14376
    Redafamdastat
    		98.86%
    Redafamdastat (PF-04457845), a chemical probe, is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.
    Redafamdastat
  • HY-N0754
    Eupalinolide A
    		Activator 99.92%
    Eupalinolide A is a Yes-associated protein (YAP) degrader and HSP70 inducer. Eupalinolide A inhibits osteogenic differentiation of tendon-derived stem cells (TDSCs). Eupalinolide A induces autophagy in hepatocellular carcinoma cells via activating the ROS/ERK signaling pathway. Eupalinolide A protects PAM212 cells from UVB-, Menadione (HY-B0332)-, or heat shock-induced apoptosis. Eupalinolide A alleviates trauma-induced heterotopic ossification (HO) of Achilles tendon and inhibits growth of MHCC97-L and HCCLM3 hepatocellular carcinoma xenograft tumors in mice. Eupalinolide A can be used for the study of traumatic heterotopic ossification of tendons and hepatocellular carcinoma.
    Eupalinolide A
  • HY-14648R
    Dexamethasone (Standard)
    		Inducer
    Dexamethasone (Standard) is the analytical standard of Dexamethasone. This product is intended for research and analytical applications. 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 (Standard)
  • HY-10181B
    Dasatinib monohydrate
    		Inducer 99.58%
    Dasatinib (BMS-354825) monohydrate is a highly potent, ATP competitive, orally active dual Src/Bcr-Abl inhibitor with potent antitumor activity. The Kis are 16 pM and 30 pM for Src and Bcr-Abl, respectively. Dasatinib monohydrate inhibits Bcr-Abl and Src with IC50s of <1.0 nM and 0.5 nM, respectively. Dasatinib monohydrate also induces apoptosis and autophagy.
    Dasatinib monohydrate
  • HY-120380
    FeTMPyP
    		Inducer 99.80%
    FeTMPyP is an orally active peroxynitrite (ONOO ) scavenger. FeTMPyP reduces nitrative stress and increases autophagy. FeTMPyP reduces PARP over-activation and neuroinflammation in chronic constriction injury (CCI)-induced rats, and ameliorates functional, behavioral and biochemical deficits.
    FeTMPyP
  • HY-B0143S2
    Niacin-d4
    		99.71%
    Niacin-d4 is the deuterium labeled Niacin. Niacin (Nicotinic acid) is a vitamin and is part of the vitamin B group.
    Niacin-d<sub>4</sub>
  • HY-10162R
    Olaparib (Standard)
    		Inducer
    Olaparib (Standard) is the analytical standard of Olaparib. This product is intended for research and analytical applications. Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
    Olaparib (Standard)
  • HY-B1839
    Fluazinam
    		Activator 99.36%
    Fluazinam is an orally active dinitroaniline fungicide. Fluazinam induces phosphorylation of JNK, activates p38 pathway, decreases Bcl-2, activates caspase-3, decreases complex I activity, increases Autophagy and Apoptosis. Fluazinam has strong antifungal activity against F. fujikuroi and B. maydis. Fluazinam has a negative impact on Brachydanio rerio and worker bees.
    Fluazinam
  • HY-12643
    Eprinomectin
    		Inducer 98.02%
    Eprinomectin (MK-397) is a type of avermectin. Eprinomectin, as a broad-spectrum fungicide, has insecticidal, insecticidal and acaricidal activities. Eprinomectin induces apoptosis and autophagy in prostate cancer cells and has antitumor activity.
    Eprinomectin
  • HY-B0165AR
    Pravastatin sodium (Standard)
    Pravastatin (sodium) (Standard) is the analytical standard of Pravastatin (sodium). This product is intended for research and analytical applications. Pravastatin sodium (CS-514 sodium) is an HMG-CoA reductase inhibitor against sterol synthesis with IC50 of 5.6 μM.
    Pravastatin sodium (Standard)
  • HY-13683R
    Mifepristone (Standard)
    		Inducer
    Mifepristone (Standard) is the analytical standard of Mifepristone. This product is intended for research and analytical applications. Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay.
    Mifepristone (Standard)
  • HY-N1458
    Isoschaftoside
    		Inducer 99.95%
    Isoschaftoside, a C-glycosylflavonoid from Desmodium uncinatum root exudate, can inhibit the growth of germinated S. hermonthica radicles. Isoschaftoside reduces reactive oxygen species (ROS) and induces proliferation in senescent cells. Isoschaftoside activates autophagy. Isoschaftoside can be used for anti-tumor, anti-inflammatory, antioxidant, antihypertensive, hepatoprotective and nematicidal study.
    Isoschaftoside
  • HY-B0319
    Tioconazole
    		Inhibitor 99.90%
    Tioconazole (UK-20349) is a broad-spectrum antifungal imidazole derivative. Tioconazole inhibits several dermatophytes and yeasts, with MIC50 values of less than 3.12 mg/L and 9 mg/L, respectively. Additionally, Tioconazole exhibits anti-parasitic activity. Tioconazole exerts anticancer activity by inhibiting the PI3K/AKT/mTOR signaling pathway and blocking autophagy. Tioconazole is applicable for research in the fields of anti-infection and anticancer therapy.
    Tioconazole
  • HY-N0353
    Curdione
    		99.92%
    Curdione ((+)-Curdione) is an orally active sesquiterpenoid. Curdione inhibits platelet aggregation. Curdione induces ferroptosis in colorectal cancer via m6A methylation mediated by METTL14 and YTHDF2. Curdione inhibits ferroptosis in Isoproterenol (HY-B0468)-induced myocardial infarction by regulating the Keap1/Trx1/GPX4 signaling pathway, suppressing oxidative stress (ROS) and apoptosis. Curdione ameliorates Doxorubicin (HY-15142)-induced cardiotoxicity by inhibiting oxidative stress (ROS) and activating the Nrf2/HO-1 pathway. Curdione ameliorates sepsis-induced lung injury by inhibiting platelet-mediated neutrophil extracellular trap formation. Curdione ameliorates Bleomycin (HY-17565A)-induced pulmonary fibrosis by inhibiting TGF-β-induced fibroblast-to-myofibroblast differentiation. Curdione exhibits neuroprotective effects against focal cerebral ischemia-reperfusion injury in rats. Curdione exerts antiproliferative effects against human uterine leiomyosarcoma by targeting IDO1. Curdione protects vascular endothelial cells and atherosclerosis by regulating DNMT1-mediated ERBB4 promoter methylation. Curdione inhibits inducible prostaglandin E2 production (IC50 = 1.1 μM) and cyclooxygenase 2 expression.
    Curdione
  • HY-18071
    BI-9627
    		99.71%
    BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
    BI-9627
Cat. No. Product Name / Synonyms Application Reactivity
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