Autophagy Signaling

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  1. anticancer agent

    Decursin is an anticancer agent, with potential anti-inflammatory activity.
  2. Apoptosis Inducer/Autophagy Inhibitor

    Kumatakenin is a potent apoptosis inducer and autophagy inhibitor that targets ATG5 with a Kd value of 2.94 μM. It effectively enhances the activity of caspases 3, 8, and 9, leading to caspase-dependent apoptosis in ovarian cancer cells while modulating chemokines and pro-oncogenic factors. Kumatakenin also reduces M2 macrophage polarization, inhibits tumor progression in esophageal cancer by targeting FASN, and interacts with Eno3 to mitigate ferroptosis and alleviate intestinal inflammation. This compound is valuable for studies in ovarian cancer, esophageal cancer, depression, and colitis research.
  3. ULK1 Inhibitor

    XST-14 is a potent and selective inhibitor of ULK1, demonstrating an IC50 of 26.6 nM. This compound effectively inhibits autophagy by decreasing the phosphorylation of ULK1 downstream substrates. XST-14 has been shown to induce apoptosis in hepatocellular carcinoma (HCC) cells, providing significant antitumor effects and contributing to ongoing cancer research and therapeutic studies.
  4. Autophagy Inducer

    Bigelovin is a sesquiterpene lactone derived from Inula hupehensis, functioning as a selective agonist of the retinoid X receptor α. It induces autophagy and apoptosis, effectively suppressing tumor growth through the inhibition of the mTOR pathway, which is modulated by reactive oxygen species (ROS) generation. This compound is valuable for research applications focused on cancer biology and the mechanisms of autophagy modulation.
  5. Autophagy Inducer

    ZPCK is a proagent of gemcitabine that functions as an autophagy inducer. It is designed to enhance oral bioavailability, facilitating more efficient delivery in research applications. ZPCK is relevant for studies exploring cancer therapies that utilize autophagy modulation to improve treatment outcomes.
  6. LRRK2 Inhibitor

    LRRK2-IN-8 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), effectively targeting both wild-type LRRK2 and the G2019S mutant with IC50 values under 10 nM. Additionally, this compound demonstrates inhibitory activity against TYK2 and NUAK1 with IC50 values ranging from 10 to 100 nM. LRRK2-IN-8 is valuable for research focused on neurodegenerative diseases linked to LRRK2, as well as studies aimed at exploring the functionality of TYK2 and NUAK1 in various cellular processes.
  7. LRRK2/NUAK1/TYK2 Inhibitor

    LRRK2/NUAK1/TYK2-IN-1 is a potent inhibitor of LRRK2, NUAK1, and TYK2, exhibiting IC50 values under 10 nM for LRRK2 (Wt), LRRK2 (G2019), TYK2, and NUAK1. This compound is valuable for research in autoimmune diseases, providing insights into the mechanisms of inflammation and immune response modulation. Its high selectivity and efficacy make it a crucial tool for studying the roles of these kinases in various biological pathways.
  8. Anticancer Agent

    Bufothionine is a natural alkaloid with anticancer properties, isolated from Cinobufacini. It induces apoptosis through a mitochondria-mediated pathway and effectively reduces serum IL-6 levels while suppressing the expression of p-Stat3tyr705, p-Stat3ser727, and Jak2. Bufothionine also promotes autophagy by upregulating key autophagy-related proteins Atg5, Atg7, and LC3Ⅱ, while inhibiting PIM3 expression. Its efficacy in preclinical models demonstrates significant anti-cancer activity against gastric cancer and highlights its potential role in therapeutic applications.
  9. ULK1/2 Inhibitor

    MR-2088 is a selective, ATP-competitive inhibitor of ULK1 and ULK2, exhibiting pEC50 values of 8.3 and 8.7, respectively. This compound effectively inhibits autophagic flux and demonstrates a synergistic antiproliferative effect with MEK inhibitors in vitro, making it a valuable tool for studying non-small cell lung cancer (NSCLC). Its ability to modulate autophagy-related pathways provides insights into cancer biology and potential therapeutic strategies.
  10. Autophagy Inducer

    Paeonol-d3 is a deuterium-labeled derivative of Paeonol, serving as an autophagy inducer. It enhances the autophagic process, which is crucial for cellular homeostasis and survival under stress conditions. This reagent is primarily utilized in studies investigating autophagy-related pathways and their implications in various diseases.
  11. Tag-Linker Conjugate

    Amino-PEG3-2G degrader-1 is a tag-linker conjugate designed to induce the ubiquitin-proteasome system (UPS) through its PEG linker and pyrazole-linked FBnG tag. This compound facilitates the synthesis of autophagy-targeting chimeras (AUTACs), enabling targeted degradation of specific cellular proteins. Its application is significant in the study of protein homeostasis and cellular degradation pathways, making it a valuable tool for research in cellular biology and therapeutic development.
  12. Autophagy Enhancer

    Valechlorine is an iridoid that functions primarily as an autophagy enhancer. It demonstrates efficacy in mitigating fatty liver conditions by promoting the breakdown of lipid droplets through autophagy. This compound is particularly useful for research involving nonalcoholic fatty liver disease (NAFLD).
  13. Autophagy Activator

    Clematichinenoside AR is an autophagy activator derived from the traditional Chinese herb Clematis chinensis. This compound exhibits significant pharmacological effects, notably in the context of atherosclerosis and related diseases. Its ability to modulate autophagy makes it a valuable tool for research into cellular processes and potential therapeutic interventions.
  14. Autophagy Inhibitor

    Autophagy-IN-5 is a potent autophagy inhibitor, exhibiting an EC50 of 0.736 μM. This compound selectively targets the autophagy pathway, playing a crucial role in cellular homeostasis and degradation processes. It is suitable for research applications investigating the modulation of autophagy in various disease contexts, including cancer and neurodegenerative disorders.
  15. Autophagy

    SLLN-15 is a potent and selective enhancer of autophagy that primarily targets the autophagic pathway. It effectively activates cytostatic macroautophagy in triple-negative breast cancer (TNBC) cells, promoting cellular degradation and recycling processes. SLLN-15 is ideal for research focused on autophagy modulation and its implications in cancer therapy, particularly in challenging malignancies like TNBC.
  16. Kif15/ULK1 Inhibitor

    (Z/E)-GW406108X serves as a selective inhibitor of Kif15, a member of the Kinesin-12 family, with an IC50 of 0.82 µM. This compound is instrumental in studying the dynamics of mitotic processes and cellular transport mechanisms. Additionally, it may have implications in cancer research, specifically in the investigation of tumor cell proliferation and migration.
  17. Autophagy

    MRT 68601 is a potent inhibitor of TBK1, predominantly influencing autophagy processes. It effectively inhibits autophagosome formation in lung cancer cells, underscoring its therapeutic potential in cancer research. Additionally, MRT 68601 may impact host-dependent factors implicated in SARS-CoV-2 infection, offering a foundation for the development of broad-spectrum antiviral therapies linked to known FDA-approved drugs and compounds currently in clinical trials.
  18. Autophagy Inducer

    Butylate is an autophagy inducer that plays a significant role in platelet research. It is involved in the activation of platelets, which can trigger autophagic processes mediated by the AMPK-MTOR signaling pathway and is associated with sphingolipid metabolism. This compound serves as a valuable tool for investigating the interplay between autophagy and metabolic pathways in hematological studies.
  19. Autophagy Inducer

    NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2), exhibiting an IC50 of 200 nM in a cell-free assay. This compound selectively inhibits Chk2 while displaying lesser activity against Brk, c-Met, IGFR, and LCK at higher concentrations. NSC 109555 disrupts Chk2 autophosphorylation and histone H1 phosphorylation with an IC50 of 240 nM. Its biological activity includes inducing autophagy and inhibiting growth in L1210 leukemia cells, as well as enhancing gemcitabine-induced cytotoxicity and increasing reactive oxygen species levels in various pancreatic cancer cell lines.
  20. Antitumor Agent

    Antitumor agent-82 is a potent antitumor compound that primarily exerts its effects through the induction of autophagy via the ATG5/ATG7 signaling pathway. This compound demonstrates significant anti-proliferative activity against various cancer cell lines, making it a valuable tool for cancer research. Antitumor agent-82 can be utilized in studies aimed at understanding autophagy's role in tumor progression and therapeutic resistance.
  21. Autophagy Inducer

    BRD5631 is an autophagy inducer that enhances the autophagic process through an mTOR-independent pathway. It has been shown to impact various cellular disease phenotypes associated with autophagy, including protein aggregation, cell survival mechanisms, bacterial replication, and the production of inflammatory cytokines. This compound is suitable for research applications exploring the roles of autophagy in disease modulation and therapeutic development.
  22. Autophagy Activator

    501A054 is an autophagy activator that promotes autophagy-dependent cell death through the activation of autophagy pathways. This compound is valuable for research applications focused on the regulation of autophagy, particularly in the context of cervical cancer studies. Its ability to induce autophagic processes makes it a significant tool for understanding cellular mechanisms and therapeutic strategies in cancer research.
  23. Autophagy Activator

    Soybean peptide QRPR is an autophagy activator that enhances cellular autophagy by increasing the expression and activity of key signaling proteins, including PIK3, AKT, and mTOR. This peptide has shown potential in reducing inflammatory responses, making it valuable for research in cellular stress responses and inflammatory diseases. Its role in modulating autophagy pathways positions it as an important tool for studies aimed at understanding cellular homeostasis and therapeutic interventions.
  24. Autophagy Inducer

    Cabergoline diphosphate is an ergot alkaloid that acts as an agonist of dopamine D2-like receptors, demonstrating high affinity for D2, D3, and 5-HT2B receptors with Ki values of 0.7, 1.5, and 1.2, respectively. It serves as an autophagy inducer, making it a valuable tool for research focused on cellular processes related to autophagy and neurobiology. This compound is instrumental in studies investigating neurodegenerative diseases and metabolic regulation, providing insights into the role of dopamine receptors in cellular homeostasis.
  25. IKKε/TBK-1 Inhibitor

    MRT67307 dihydrochloride is a potent inhibitor of IKKε and TBK-1, demonstrating IC50 values of 160 nM and 19 nM, respectively. Additionally, this compound inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. MRT67307 dihydrochloride plays a significant role in blocking autophagy in cellular environments, making it a valuable tool for studies involving inflammation and autophagic processes.
  26. Autophagy

    Calmodulin-Dependent Protein Kinase II (290-309) is a specific antagonist of CaMK with a reported IC50 of 52 nM, effectively inhibiting calmodulin-dependent protein kinase II activity. This reagent plays a crucial role in the study of autophagy, facilitating research into cellular signaling pathways regulated by calcium and calmodulin. It is valuable for investigating the physiological and pathological processes influenced by CaMKII, providing insights into various diseases and potential therapeutic targets.
  27. Autophagy Inducer

    Autophagonizer (DK-1-49) is a small molecule autophagy inducer that promotes the accumulation of autophagy-associated LC3-II while increasing the levels of autophagosomes and acidic vacuoles. This compound effectively inhibits cell viability and induces cell death in cancer cells as well as Bax/Bak double-knockout cells, demonstrating EC50 values of 3-4 μM. Autophagonizer serves as a valuable tool for research into autophagy-related processes and potential therapeutic interventions in cancer biology.
  28. Autophagy Inhibitor

    ATG12-IN-1 is an autophagy inhibitor that effectively disrupts the ATG12-ATG3 protein-protein interaction, exhibiting an IC50 of 9 μM. This compound is valuable in cancer research, allowing for the exploration of autophagy dynamics and its implications in tumor biology. It provides a robust tool for investigating the role of autophagy in cancer progression and therapeutic resistance.
  29. Autophagy-Targeting Chimera

    2G-HaloAUTAC is a second-generation autophagy-targeting chimera designed to enhance the efficacy of AUTACs by substituting the L-Cysteine linker with alternative structures. This compound demonstrates potent degradation activity against EGFP-HaloTag protein via an autophagic mechanism. It serves as a valuable tool for research focused on autophagy and targeted protein degradation, providing insights into cellular protein turnover processes.
  30. Autophagy Inhibitor

    Autophagy-IN-4 (Compound 34) is a potent autophagy inhibitor, demonstrating an EC50 of 0.5 μM in U2OS cells and an LD50 of 27 μM. This compound effectively interferes with the autophagic process, making it a valuable tool for researchers investigating the role of autophagy in various biological contexts and disease models. Its specificity and efficacy support its application in studies aimed at understanding autophagy-related pathways and potential therapeutic interventions.
  31. Autophagy Inhibitor

    Autophagy-IN-3 is an autophagy inhibitor that enhances metabolic stress within the tumor microenvironment. By inhibiting autophagic processes, it significantly increases the efficacy of cytostatics in combination therapies. This compound is particularly valuable in cancer research, where modulating autophagy can influence tumor growth and treatment response.
  32. Autophagy Inducer

    CR-3294 is an autophagy inducer that specifically targets hypoxic cells by inhibiting inducible nitric oxide synthase (iNOS). It effectively inhibits the DNA binding activity of HIF-1alpha and reduces VEGF mRNA synthesis. This compound is valuable for research applications involving breast cancer and inflammatory bowel diseases (IBD), including Crohn's disease and ulcerative colitis, by elucidating the role of autophagy in these conditions.
  33. Autophagy Inducer

    SMER10 is a small-molecule autophagy inducer that enhances the formation of autophagosomes. This compound promotes the conversion of LC3-I to the autophagosome-associated form, LC3-II, thereby increasing the number of EGFP-LC3 positive structures in COS-7 and HeLa cells. SMER10 has been shown to facilitate the degradation of autophagic substrates such as the mutant huntingtin protein (EGFP-HDQ74) linked to Huntington's disease and A53T α-synuclein associated with Parkinson's disease, demonstrating its neuroprotective properties in relevant cellular models.
  34. Tag-Linker Conjugate

    FBnG-amino-PEG3-C2-azido is a tag-linker conjugate designed to facilitate targeted protein degradation. It combines the degradation tag FBnG with a glycol linker, Amino-PEG3-C2-azido, to enhance the selective degradation of target proteins. This reagent enables the synthesis of GPX4-AUTAC and is valuable in studies of protein homeostasis and cellular responses to stress. Its versatile application is important for researchers investigating targeted therapeutic strategies in various biological contexts.
  35. Autophagy Inducer

    Isodunnianol is a novel autophagy inducer that enhances autophagic activity by increasing the expression of pAMPK172 and pULK1555 while simultaneously reducing levels of pULK1757 and SQSTM2. This compound has demonstrated the ability to mitigate doxorubicin-induced cardiotoxicity, making it a valuable tool for research in cardioprotection and autophagy-related pathways. Its application can further advance studies related to cancer therapy and cellular stress responses.
  36. Autophagy Inducer

    Amsacrine (gluconate) is an inhibitor of topoisomerase II, primarily functioning as an autophagy inducer. This compound exhibits significant antineoplastic activity by intercalating into the DNA of tumor cells, disrupting their replication and promoting cell death. Amsacrine (gluconate) is commonly utilized in cancer research to explore mechanisms of tumor growth inhibition and the roles of autophagy in cancer treatment.
  37. Autophagy Inducer

    Chromomycin A2 is an autophagy inducer known for its cytotoxic properties. This compound exhibits significant anti-tumor activity, making it a valuable tool in cancer research. Its ability to modulate autophagy pathways allows for investigation into cancer cell survival and proliferation, facilitating studies focused on therapeutic interventions.
  38. Autophagy Activator

    AR493 is an autophagy activator that targets AMPK (adenosine monophosphate-activated protein kinase). It modulates pathways involved in cellular energy sensing, leading to increased levels of autophagy. This compound is valuable for research into aging-associated disorders, including diabetes and neurodegenerative diseases, as well as for studies on autophagy regulation.
  39. Antitumor Agent

    Antitumor agent-199 is an antitumor compound that demonstrates significant antiproliferative effects across various tumor cell lines. It effectively induces autophagy in cancer cells by activating the ATG5/ATG7 pathway. This agent is valuable for research applications focused on cancer biology and therapeutic development.
  40. ATG4B Inhibitor

    MJO445 is a selective inhibitor of ATG4B, a key regulator in the autophagy pathway. Its inhibition of ATG4B disrupts the autophagic process in glioblastoma cells, thereby enhancing the efficacy of therapeutic strategies against this aggressive cancer. MJO445 is particularly relevant for research focused on cancer biology, autophagy modulation, and the development of novel cancer treatments.
  41. Autophagy Inhibitor

    Autophagy-IN-C1 is a potent autophagy inhibitor that effectively inhibits the autophagic process in hepatocellular carcinoma (HCC) cells. In addition to its role in blocking autophagy, this compound also induces apoptosis, making it a valuable tool for investigating cell death mechanisms and therapeutic strategies in cancer research. Its dual activity provides insights into the interplay between autophagy and apoptosis in tumor biology.
  42. ULK1/ULK2 Inhibitor

    SBP-5147 is a potent inhibitor of ULK1 and ULK2, exhibiting an IC50 of 2 nM for ULK1 and 53 nM for ULK2. This compound effectively inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagic flux, and downregulates the expression of key autophagy-related proteins ATG13 and ATG101. Additionally, SBP-5147 enhances MHC-I expression, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. Its mechanism of action makes SBP-5147 a valuable tool for research in non-small cell lung cancer and autophagy modulation.
  43. Autophagy Inhibitor

    Autophagy-IN-7 is an autophagy inhibitor that targets the autophagic process in cells. It is primarily utilized in cancer research to investigate the effects of autophagy modulation on tumor progression and treatment response. This compound serves as a valuable tool for elucidating the role of autophagy in various cellular mechanisms and cancer biology.
  44. Autophagy

    (1R)-cis-Bifenthrin is a synthetic pyrethroid that targets autophagy pathways, particularly affecting motor coordination. Research indicates that (1R)-cis-Bifenthrin exposure leads to decreased motor function in ParKin-/- mice, evidenced by prolonged pole climbing times and reduced wheel running activity. The compound significantly decreases the number of tyrosine hydroxylase-positive cells and alters protein expression levels. Notably, (1R)-cis-Bifenthrin promotes the expression of mitophagy-related proteins, including LC3B and p62, while demonstrating enhanced binding affinity for transferrin and transferrin receptor 2. These interactions underscore its role in mitophagy and ferroptosis-related signaling pathways.
  45. Autophagy Inducer

    8-Nitro-cGMP is an electrophilic second messenger involved in redox signaling that acts through the formation of protein-S-cGMP adducts via the s-guanylation process. This compound serves as an inducer of autophagy, demonstrating significant biological activity in promoting RANKL-induced osteoclast differentiation from macrophages. Additionally, 8-Nitro-cGMP exhibits vasodilatory effects and has been shown to improve vascular endothelial dysfunction in diabetic mouse models, making it a valuable tool for research in cellular signaling and metabolic disorders.
  46. Autophagy

    SW063058 is an autophagy inducer that selectively disrupts the interaction between Beclin 1 and Bcl-2, while preserving the binding of Bcl-2 to pro-apoptotic proteins such as Bax and BIM. This selective inhibition relieves the negative regulatory effects of Bcl-2 on Beclin 1, thereby enhancing autophagic activity. SW063058 promotes autophagy in vitro without inducing cytotoxicity, apoptosis, or other forms of cell death, making it a valuable tool for studying autophagic processes in various biological contexts.
  47. Autophagy Inhibitor

    CP 53631 is an autophagy inhibitor that demonstrates anticancer activity by disrupting the autophagic process in cancer cells. This compound can also serve as an internal standard in studies examining selective serotonin reuptake inhibitors (SSRIs) such as Sertraline, making it valuable for research in antidepressant mechanisms and effects. Its dual applications in oncology and neuropharmacology underscore its significance in advancing both fields.
  48. TbCATL Inhibitor

    CAA-0225 is a selective inhibitor of the tissue protease L, specifically targeting TbCATL with an IC50 of 1.9 nM. This compound has demonstrated significant biological activity, including the degradation of autophagosome membrane markers such as LC3-II and GABARAP. Additionally, CAA-0225 improves cardiac function in models of reperfusion injury and exhibits efficacy against Trypanosoma brucei, highlighting its potential applications in cardiovascular research and parasitology studies.
  49. Autophagy Activator

    Autophagy activator-1 is an autophagy enhancer that promotes the autophagic process by downregulating significant members of the HSP70 family while simultaneously activating the unfolded protein response. This compound serves as a valuable tool in research focused on cellular degradation pathways, protein homeostasis, and conditions associated with autophagy dysregulation. Its application extends to studies involving neurodegenerative diseases, cancer biology, and metabolic disorders.
  50. Antagonist

    Peptide E5 is an antagonist that targets the CXCR4/CXCL12 signaling axis. By blocking this interaction, Peptide E5 downregulates CXCR4 expression and inhibits the phosphorylation of key downstream proteins, Akt and Erk, leading to apoptosis in breast cancer cells. Additionally, Peptide E5 suppresses cellular migration and adhesion, as well as the recruitment of endothelial progenitor cells, thereby inhibiting tumor angiogenesis. This peptide is a valuable tool for research related to breast cancer and tumor microenvironment interactions.

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