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-164468
    Ch282-5
    Ch282-5 is an orally active inhibitor targeting the Bcl-2 protein, inducing mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. Ch282-5 exhibits antiproliferative activity against colorectal cancer cells both in vitro and in vivo, and it also inhibits metastasis. Additionally, Ch282-5 enhances Oxaliplatin (HY-17371)-induced autophagy (Autophagy) by downregulating the Mcl-1 protein and increasing platelet count, alleviating adverse effects of Navitoclax (HY-10087).
    Ch282-5
  • HY-B0102S
    Fluoxetine-d6
    		Inducer
    Fluoxetine-d6 (LY-110140 (free base)-d6) is deuterium labeled Fluoxetine. Fluoxetine (LY-110140 free base) is a selective serotonin reuptake inhibitor (SSRI) class used for antidepressant research.
    Fluoxetine-d<sub>6<sub>
  • HY-10585AG
    Valproic acid (sodium) (GMP)
    		Inducer
    Valproic acid (Sodium Valproate) sodium is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid sodium activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid sodium is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches.
    Valproic acid (sodium) (GMP)
  • HY-W653970
    5-Azacytidine-15N4
    		Inducer
    5-Azacytidine-15N4 is 13C and 15N labeled 5-Azacytidine. 5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes. 5-Azacytidine induces cell autophagy.
    5-Azacytidine-<sup>15</sup>N<sub>4</sub>
  • HY-16562R
    Irinotecan (Standard)
    		Inducer
    Irinotecan (Standard) is the analytical standard of Irinotecan. This product is intended for research and analytical applications. Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
    Irinotecan (Standard)
  • HY-100490AR
    Rilmenidine hemifumarate (Standard)
    		Inducer
    Rilmenidine (hemifumarate) (Standard) is the analytical standard of Rilmenidine (hemifumarate). This product is intended for research and analytical applications. Rilmenidine hemifumarate, an innovative antihypertensive agent, is an orally active, selective I1 imidazoline receptor agonist. Rilmenidine hemifumarate is an alpha 2-adrenoceptor agonist. Rilmenidine hemifumarate induces autophagy. Rilmenidine hemifumarate acts both centrally by reducing sympathetic overactivity and in the kidney by inhibiting the Na+/H+ antiport. Rilmenidine hemifumarate modulates proliferation and stimulates the proapoptotic protein Bax thus inducing the perturbation of the mitochondrial pathway and apoptosis in human leukemic K562 cells .
    Rilmenidine hemifumarate (Standard)
  • HY-13017S4
    Ivacaftor-13C6
    Ivacaftor-13C6 (VX-770-13C6) is 13C labeled Ivacaftor. Ivacaftor (VX-770) is a potent and orally bioavailable CFTR potentiator, targeting G551D-CFTR and F508del-CFTR with EC50s of 100 nM and 25 nM, respectively.
    Ivacaftor-<sup>13</sup>C<sub>6</sub>
  • HY-17507R
    Pantoprazole (Standard)
    		Inhibitor
    Pantoprazole (Standard) is the analytical standard of Pantoprazole. This product is intended for research and analytical applications. Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H+/K+-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
    Pantoprazole (Standard)
  • HY-W779021
    Adenosine-15N
    		Inducer
    Adenosine-15N (Adenine riboside-15N) is 15N labeled Adenosine. Adenosine (Adenine riboside), a ubiquitous endogenous autacoid, acts through the enrollment of four G protein-coupled receptors: A1, A2A, A2B, and A3. Adenosine affects almost all aspects of cellular physiology, including neuronal activity, vascular function, platelet aggregation, and blood cell regulation.
    Adenosine-<sup>15</sup>N
  • HY-B0107A
    Acitretin sodium
    Acitretin (Ro 10-1670) sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. Acitretin sodium also can be used for the research of Alzheimer’s disease.
    Acitretin sodium
  • HY-N14738
    Dutomycin
    		Inducer
    Dutomycin is a SERPINB6 inhibitor with a binding constant (KD) of 1.236 μM. Dutomycin can induce autophagy and apoptosis in cancer cells and inhibit the growth of cancer cells in a zebrafish xenograft model. Dutomycin is promising for research of cancers.
    Dutomycin
  • HY-13704R
    SN-38 (Standard)
    		Inducer
    SN-38 (Standard) is the analytical standard of SN-38. This product is intended for research and analytical applications. SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively. SN-38 is a payload of sacituzumab govitecan (HY -132254).
    SN-38 (Standard)
  • HY-13757R
    Tamoxifen (Citrate) (Standard)
    		Inducer
    Tamoxifen (Citrate) (Standard) is the analytical standard of Tamoxifen (Citrate). This product is intended for research and analytical applications. Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.
    Tamoxifen (Citrate) (Standard)
  • HY-13551R
    Amsacrine (Standard)
    		Inducer
    Amsacrine (Standard) is the analytical standard of Amsacrine. This product is intended for research and analytical applications. Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells.
    Amsacrine (Standard)
  • HY-10201AR
    Sorafenib (tosylate) (Standard)
    		Inducer
    Sorafenib tosylate (Standard) is the analytical standard of Sorafenib tosylate. This product is intended for research and analytical applications. Sorafenib tosylate (Bay 43-9006 tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. Sorafenib tosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib tosylate is a ferroptosis activator.
    Sorafenib (tosylate) (Standard)
  • HY-50878S1
    Crizotinib-d8
    		Inducer
    Crizotinib-d8 (PF-02341066-d8) is deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition.
    Crizotinib-d<sub>8</sub>
  • HY-16508S1
    Ulipristal acetate-d3
    		Inducer
    Ulipristal acetate-d3 (CDB-2914-d3) is deuterium labeled Ulipristal acetate. Ulipristal acetate (CDB-2914) is an orally active, selective progesterone receptor modulator (SPRM). Ulipristal acetate stimulates the autophagic response selectively in leiomyoma cells. Ulipristal acetate has the potential for benign gynecological conditions treatment, such as uterine myoma.
    Ulipristal acetate-d<sub>3</sub>
  • HY-10562R
    Ketanserin (Standard)
    		Inducer
    Ketanserin (Standard) is the analytical standard of Ketanserin. This product is intended for research and analytical applications. Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
    Ketanserin (Standard)
  • HY-B0803R
    Lumefantrine (Standard)
    		Inhibitor
    Lumefantrine (Standard) is the analytical standard of Lumefantrine. This product is intended for research and analytical applications. Lumefantrine is an active antimalarial molecule used in combination with Artemether as a first- and second-line antimalarial drug.
    Lumefantrine (Standard)
  • HY-W653875
    Azithromycin-d5
    		Inhibitor
    Azithromycin-d5 (CP-62993-d5) is the deuterium labeled Azithromycin (CP-62993) (HY-17506). Azithromycin is a macrolide antibiotic useful for thestudy of a number of bacterial infections.
    Azithromycin-d<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity
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