Autophagy Signaling

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  1. IKKε/TBK-1 Inhibitor

    MRT67307 hydrochloride is a selective inhibitor of IKKε and TBK-1, exhibiting IC50 values of 160 nM and 19 nM, respectively. Additionally, it inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. This compound is employed in research to study autophagy regulation and related cellular processes. It is particularly useful in investigations of inflammatory signaling pathways and cancer biology.
  2. Autophagy Inducer

    Atorvastatin-d5 sodium is a deuterium-labeled analog of atorvastatin, an oral HMG-CoA reductase inhibitor. This compound effectively lowers blood lipid levels and acts as an autophagy inducer. It has been shown to inhibit human smooth muscle cell proliferation and invasion, with IC50 values of 0.39 μM and 2.39 μM, respectively. Atorvastatin-d5 sodium is valuable for research applications related to lipid metabolism and cellular growth regulation.
  3. REV-ERB/Autophagy Inhibitor

    ARN5187 is a lysosomotropic ligand targeting REV-ERBβ, known for its dual inhibitory effects on REV-ERB-mediated transcriptional regulation and autophagy. This compound exhibits significant lysosomotropic potency and has cytotoxic properties, leading to the induction of apoptosis. ARN5187 serves as a valuable tool for research into the mechanisms of autophagy and the role of REV-ERBβ in cellular processes.
  4. Autophagy Inducer

    SGI-1776 is a selective inhibitor of Pim kinases, exhibiting IC50 values of 7 nM for Pim-1, 363 nM for Pim-2, and 69 nM for Pim-3. This compound has been identified as an autophagy inducer, showcasing potential mechanisms in cellular pathways associated with cancer and metabolic disorders. SGI-1776 is employed in research applications focusing on the modulation of cell survival and proliferation, making it a valuable tool for investigating therapeutic strategies targeting the Pim kinase signaling network.
  5. Autophagy Inhibitor

    IITZ-02 is a lysosomotropic autophagy inhibitor that disrupts lysosomal function, leading to impaired autophagosomal degradation and increased autophagosome accumulation. This compound induces apoptosis through a mitochondria-mediated pathway by abolishing mitochondrial membrane potential. IITZ-02 exhibits potent antitumor activity in MDA-MB-231 xenograft mouse models, making it a valuable tool for cancer research applications focusing on the regulation of autophagy.
  6. CXCR-4 Inhibitor

    SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions.
  7. Autophagy Inhibitor

    Erythrabyssin II is a potent late-stage autophagy inhibitor that selectively inhibits the fusion of autophagosomes and lysosomes. This compound promotes the accumulation of autophagic substrates without disrupting lysosomal pH or enzyme activity. Erythrabyssin II has demonstrated efficacy in suppressing ovarian cancer organoid growth and inducing apoptosis, making it a valuable tool for research in ovarian cancer studies.
  8. Autophagy Inhibitor

    EAD1 TFA is an autophagy inhibitor that plays a critical role in the regulation of plant growth and development, particularly in maize. This compound is preferentially expressed in the xylem of immature corn ears, where it facilitates the transport of malic acid. Its function is essential for proper ear length and kernel development, with alterations in EAD1 TFA expression correlating with changes in malic acid content. EAD1 TFA represents a valuable tool for researchers investigating the genetic basis of crop yield improvement.
  9. Autophagy Inducer

    Imipramine-d4-1 is a deuterated derivative of Imipramine, primarily targeting autophagy induction. It exhibits significant antitumor activity through inhibition of Fascin1 and has a notable effect on serotonin transporter with an IC50 value of 32 nM. In cellular assays, Imipramine-d4-1 has been shown to stimulate autophagy in U-87MG glioma cells and induce apoptosis in HL-60 cells. Additionally, it demonstrates neuroprotective and immunomodulatory properties, making it valuable for various research applications in cancer biology and neurobiology.
  10. Autophagy Enhancer

    IR-58 is a mitochondria-targeting near-infrared fluorophore that enhances autophagy. It effectively induces apoptosis in tumor cells by promoting excessive autophagy through the activation of the reactive oxygen species (ROS)-Akt-mTOR signaling pathway. This compound is valuable for research applications focused on cancer biology, autophagy modulation, and therapeutic development.
  11. Anticancer Agent

    Tubulosine is an alkaloid that functions as a selective inhibitor of the Janus kinase 3 (JAK3) with an IC50 of 9.9 nM. It exhibits enhanced inhibition of JAK3 compared to other JAK family members, with IC50 values of 69.5 nM for JAK1, 84.9 nM for JAK2, and 76.3 nM for TYK2. Tubulosine induces both apoptotic and necrotic/autophagic cell death in cancer cells and disrupts peptide chain elongation in eukaryotic polysomes. This compound demonstrates promising anticancer activity, particularly in breast cancer cell lines, making it a valuable tool for cancer research.
  12. Autophagy Inducer

    Autophagy Inducer 2 is a potent activator of autophagy, primarily targeting cellular mechanisms involved in this critical survival process. It demonstrates significant antiproliferative effects on MCF-7 breast cancer cells, with an IC50 value of 1.31 μM, and markedly reduces colony formation in these cells. By modulating cell-cycle-related proteins such as Cdk-1 and Cyclin B1, Autophagy Inducer 2 effectively induces cell cycle arrest in the G2/M phase. This compound offers valuable insights for research in breast cancer therapy and the regulation of autophagy.
  13. Autophagy Inhibitor/Ionic Compound

    Ammonium chloride is an ionic compound known for its role as an autophagy inhibitor. By inducing intracellular alkalization, it can disrupt lysosomal function and alter enzymatic activity, leading to metabolic acidosis. This compound is widely utilized in research applications focused on autophagy modulation and lysosomal pathway studies.
  14. Autophagy Inhibitor; p62 ZZ Domain Inhibitor

    XRK3F2 is a selective inhibitor of the p62 (sequestosome-1) ZZ domain, demonstrating potent inhibition of autophagy processes. This compound effectively blocks TNFα-induced signaling in bone marrow stromal cells and promotes apoptosis in multiple myeloma cells. XRK3F2 is valuable for research applications targeting multiple myeloma bone disease and acute myeloid leukemia, providing insights into cell survival mechanisms and autophagic regulation in hematological malignancies.
  15. Autophagy Inducer

    Eupatilin is a lipophilic flavonoid extracted from Artemisia argyi Lévl. et Van. that acts as an autophagy inducer and PPARα agonist. It demonstrates significant anti-apoptotic, anti-oxidative, and anti-inflammatory activities. This compound is valuable for research in cellular stress responses, inflammation, and neuroprotection studies.
  16. Cytokinin Nucleoside/Autophagy Inhibitor

    N6-Isopentenyladenosine, a cytokinin nucleoside, acts primarily as an autophagy inhibitor. This compound, derived from the mevalonate pathway, has demonstrated notable anti-melanoma activity. Additionally, it plays a critical role in RNA modification, enhancing the efficiency and accuracy of translation in certain tRNAs and regulating plant growth and differentiation. Research applications include investigations into autophagy-related mechanisms and the development of therapeutic strategies for melanoma.
  17. Autophagy Inducer

    Oxyresveratrol is a potent autophagy inducer with significant antioxidant properties, exhibiting an IC50 of 28.9 µM against DPPH free radicals. It serves as a noncompetitive inhibitor of tyrosinase, demonstrating an IC50 value of 1.2 µM for mushroom tyrosinase. Oxyresveratrol has been shown to exhibit antiviral activity against HSV-1, HSV-2, and varicella-zoster virus, as well as providing neuroprotective effects. This compound is valuable for research into cellular protection mechanisms and the regulation of metabolic processes.
  18. Autophagy Inducer

    BGT226 is a dual inhibitor targeting PI3K and mTOR, demonstrating IC50 values of 4 nM, 63 nM, and 38 nM against PI3Kα, PI3Kβ, and PI3Kγ, respectively. This compound effectively induces autophagy, showcasing significant growth-inhibitory effects in human head and neck cancer cells. BGT226 is valuable for research in cancer biology and drug development focused on autophagy modulation and PI3K/mTOR signaling pathways.
  19. ATG7 Inhibitor

    ATG7-IN-2 is a potent inhibitor of ATG7, demonstrating an IC50 of 0.089 μM. This compound effectively inhibits the autophagy marker LC3B, making it a valuable tool for studies involving autophagy modulation. Researchers can utilize ATG7-IN-2 to investigate the role of autophagy in various biological processes and disease states.
  20. Autophagy Inhibitor

    DC-LC3in-D5 functions as an autophagy inhibitor by inhibiting the lipidation of LC3B. It effectively binds to LC3B and disrupts the interaction with LBP2, exhibiting an IC50 value of 200 nM. This compound is valuable in research focused on the modulation of autophagy, contributing to investigations of anti-HCV therapies and potential cancer treatments through autophagy inhibition.
  21. Autophagy Inducer

    Sedanolide is a natural compound recognized for its role as an autophagy inducer. This compound exhibits significant anti-inflammatory and antioxidant properties, making it valuable in various biological research applications. Its ability to modulate cellular processes associated with autophagy allows researchers to explore its potential therapeutic effects in diseases linked to autophagic dysfunction.
  22. Autophagy Activator

    Ginkgolide K is an autophagy activator derived from Ginkgo biloba. It stimulates protective autophagy by modulating the AMPK/mTOR/ULK1 signaling pathway, thereby promoting cellular survival. Additionally, Ginkgolide K exhibits neuroprotective properties, making it a valuable tool for research in neurobiology and cellular stress responses.
  23. Autophagy Inducer

    Pyriproxyfen acts as a juvenile hormone analog, primarily targeting larval development by inhibiting the transition to adulthood. This mechanism effectively reduces reproductive capabilities in various insect species. Pyriproxyfen is widely utilized in chemical research to study autophagy induction and its implications in pest control and developmental biology.
  24. Autophagy Inhibitor

    ATG7-IN-1 is a selective inhibitor of the autophagy-related protein ATG7, exhibiting an IC50 of 62 nM. This compound interferes with autophagy processes by disrupting the function of ATG7, making it a valuable tool for research in autophagy regulation. It is particularly useful for studies investigating the role of autophagy in various diseases, including cancer and neurodegenerative disorders.
  25. Autophagy Inducer

    Pemetrexed disodium heptahydrate is an innovative antifolate that serves as an autophagy inducer. It effectively inhibits key enzymes including thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), with Ki values of 1.3, 7.2, and 65 nM, respectively. This compound is valuable in research applications targeting metabolic pathways and autophagic processes in cancer and other diseases.
  26. Autophagy Inhibitor

    Autogramin-2 is a potent autophagy inhibitor that effectively blocks autophagy triggered by nutrient deprivation, demonstrating an IC50 of 0.27 μM, as well as autophagy induced by mTORC1 inhibition with Rapamycin, with an IC50 of 0.14 μM. This compound is valuable for studying the role of autophagy in cellular processes and various diseases, including cancer and neurodegeneration. Its ability to modulate autophagic pathways makes it an essential tool for researchers investigating autophagy's impact on cell survival and metabolism.
  27. Autophagy Inducer

    XIE62-1004-A is a potent inducer of p62-LC3 interaction, specifically targeting the ZZ-domain of p62. Its binding induces p62 oligomerization, thereby activating p62-dependent autophagy processes. This compound is valuable for research applications investigating the mechanisms of autophagy and its role in cellular homeostasis and disease.
  28. Autophagy Inducer

    AMDE-1 is a potent autophagy inducer that activates the AMPK-mTORC1-ULK1 signaling pathway. While promoting autophagy, AMDE-1 also disrupts lysosomal function, thereby inhibiting autophagy-mediated degradation. This dual mechanism makes AMDE-1 a valuable tool for investigating autophagy-related processes in cancer research.
  29. Autophagy Inducer

    Paroxetine hydrochloride hemihydrate is a selective serotonin reuptake inhibitor that also functions as an autophagy inducer. With an IC50 of 14 μM for GRK2 inhibition, it demonstrates potential in neuroprotective research and the study of mood disorders. This compound is suitable for investigations into its effects on cellular processes such as autophagy, neurobiology, and therapeutic applications for depression.
  30. Kif15/ULK1 Inhibitor

    GW406108X is a selective inhibitor of Kif15 (Kinesin-12) and exhibits a significant inhibition of ULK1 kinase activity with a pIC50 of 6.37 (427 nM). This compound demonstrates potent autophagy inhibition, effectively blocking autophagic flux without impacting upstream signaling pathways such as mTORC1 and AMPK. GW406108X serves as a valuable tool in research focusing on autophagy regulation and related cellular processes.
  31. ATG7 Inhibitor

    ATG7-IN-3 is a highly effective inhibitor of ATG7, exhibiting an IC50 of 0.048 μM. This compound disrupts autophagy by preventing the formation of LC3B puncta, a critical process in the autophagic pathway. Research applications include investigations into glioma and colon cancer, making it a valuable tool for studying the role of autophagy in cancer biology.
  32. Autophagy Inducer

    20-Deoxyingenol is a diterpene compound identified from the roots of Euphorbia kansui, known for its role as an autophagy inducer. This compound promotes autophagy and lysosomal biogenesis by facilitating the nuclear translocation of transcription factor EB (TFEB) in vitro. 20-Deoxyingenol is valuable for research into osteoarthritis (OA) and other conditions related to autophagy modulation.
  33. Autophagy Inducer

    Asperphenamate is an autophagy inducer derived from the fungal metabolite Aspergillus flatiipes, known for its anti-cancer properties. It demonstrates potent cytotoxic effects, with IC50 values of 92.3 μM in T47D cells, 96.5 μM in MDA-MB-231 cells, and 97.9 μM in HL-60 cells. This compound is valuable in cancer research for exploring autophagy modulation and evaluating therapeutic strategies targeting tumor cell survival.
  34. mTOR Inhibitor/Autophagy Inducer

    mTOR inhibitor-8 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), functioning through the interaction with FKBP12. This compound effectively suppresses mTOR activity and induces autophagy in A549 human lung cancer cells. It is a valuable tool for studying mTOR signaling pathways and the role of autophagy in cancer research.
  35. Autophagy Inducer

    C16 PEG2000 Ceramide is a polyethylene glycolylated ceramide that serves as an autophagy inducer. This compound promotes cellular autophagy processes, making it a valuable tool in cancer research. Additionally, C16 PEG2000 Ceramide can be utilized as a lipid carrier for targeted delivery of therapeutic agents in various experimental applications.
  36. Autophagy Inducer

    Autophagy Inducer 3 is an agent that promotes autophagy through the induction of lethal autophagic processes. It has been shown to effectively induce autophagic cell death in various cancer cell lines while sparing normal cells. The compound triggers the formation of characteristic autophagic vacuoles and LC3 puncta, along with the upregulation of key autophagy-related markers such as Beclin and members of the Atg protein family, making it valuable for research in cancer biology and autophagy modulation.
  37. Autophagy Enhancer

    AUTEN-67 is an orally active autophagy enhancer that also functions as an inhibitor of MTMR14. This compound exhibits significant anti-aging and neuroprotective properties, effectively protecting neurons from stress-induced cell death. Additionally, AUTEN-67 has been shown to restore nesting behavior in mouse models of Alzheimer’s disease, making it a valuable tool for researchers studying neurodegenerative disorders and autophagy modulation.
  38. PD-L1 Ligand

    2-Methylbiphenyl-oxadiazole-NH-Ph-CHO functions as a ligand for PD-L1, playing a crucial role in the development of AUTAC PD-L1 degrader-3. This compound is essential for facilitating targeted degradation of PD-L1, making it a valuable tool in cancer immunotherapy research and studies focusing on the modulation of immune checkpoints. Additionally, it can be utilized in the synthesis of AUTACs for advanced therapeutic applications.
  39. CXCR2 Agonist

    Ac-Pro-Gly-Pro-OH acts as a CXCR2 agonist and is an endogenous degradation product of extracellular collagen. This compound demonstrates significant bactericidal activity through hydrogen peroxide generation and plays a role in inhibiting pulmonary inflammation while reducing immune cell apoptosis. Ac-Pro-Gly-Pro-OH promotes the secretion of IFN-γ and suppresses the levels of pro-inflammatory cytokines such as TNF-α and IL-6 in leukocytes. It is relevant for research applications in sepsis, chronic obstructive pulmonary disease, cystic fibrosis, bronchiolitis obliterans syndrome, severe asthma, idiopathic pulmonary fibrosis, and corneal ulcers, notably influencing neutrophil behavior and tissue remodeling processes.
  40. CXCR2 Antagonist

    Elubrixin tosylate is a selective and reversible antagonist of the CXCR2 receptor, functioning as an IL-8 receptor antagonist. This compound effectively inhibits neutrophil CD11b upregulation with an IC50 of 260.7 nM and neutrophil shape change with an IC50 of 310.5 nM. Its biological activity positions Elubrixin tosylate as a valuable tool in research aimed at understanding and treating inflammatory diseases, including inflammatory bowel disease and airway inflammation.
  41. CXCR2 Antagonist

    Elubrixin is a potent and selective CXCR2 antagonist, functioning as a competitive and reversible inhibitor of the IL-8 receptor. It effectively impedes neutrophil CD11b upregulation with an IC50 of 260.7 nM and inhibits shape change with an IC50 of 310.5 nM. This compound is valuable in the study of inflammatory diseases, including inflammatory bowel disease and airway inflammation, facilitating insights into pathophysiological mechanisms and therapeutic interventions.
  42. CXCR2 Antagonist

    Elubrixin hydrochloride is a potent, selective CXCR2 antagonist that operates as a competitive, reversible inhibitor of the IL-8 receptor. It effectively inhibits neutrophil CD11b upregulation and shape change, with an IC50 of 260.7 nM and 310.5 nM, respectively. This compound is valuable for research applications related to inflammatory diseases, including inflammatory bowel disease and airway inflammation.
  43. CXCR4 Antagonist

    Burixafor hydrobromide is a potent CXCR4 antagonist with a pIC50 of 7.4, effectively inhibiting the binding of CXCL12 to the CXCR4 receptor. This compound antagonizes CXCL12-induced recruitment of Gαᵢ and β-arrestin2, thereby obstructing the downstream Gαᵢ-mediated inhibition of cAMP signaling. Burixafor hydrobromide is utilized in research for mobilizing CD34+ hematopoietic stem/progenitor cells from the bone marrow to peripheral blood, making it valuable in studies related to autologous hematopoietic stem cell transplantation.
  44. LRRK2 Inhibitor

    LRRK2-IN-17 is a potent inhibitor of Leucine-rich repeat kinase 2 (LRRK2), with IC50 values of 3.5 nM and 3.3 nM for wild-type and G2019S mutant variants, respectively. Additionally, it exhibits inhibitory activity against RET kinase with an IC50 of 59 nM. This compound is relevant for research applications related to cancer and Parkinson's disease, making it a valuable tool for investigating the role of LRRK2 in these conditions.
  45. RDC-related Molecule

    NOTA-NHS ester is a chelating agent that allows for the creation of radiolabeled compounds, specifically through coupling with T140 to form NOTA-T140. This compound can then be radiolabeled with Al[18F], enabling visualization of tumor uptake that correlates with CXCR4 expression levels. Al[18F]NOTA-T140 is particularly valuable for PET imaging studies of tumors. Additionally, NOTA-NHS ester serves as a versatile tool for fluorescent labeling in various biological applications.
  46. CXCR4 Targeting Peptide

    Pentixafor is a synthetic peptide that targets the CXCR4 receptor, playing a critical role in various cellular processes, including cell migration and signaling. This compound can be labeled with 68Gallium (68Ga), enabling its application in positron emission tomography (PET) imaging for assessing CXCR4 expression in vivo. Additionally, Pentixafor serves as a vital component in the development of Radionuclide-Drug Conjugates (RDCs) for targeted cancer therapies.
  47. Endoradiotherapeutic vector

    Anditixafortide is a CXCR4-targeting peptide derivative that functions as an endoradiotherapeutic vector. This reagent is primarily utilized in the synthesis and research of Radionuclide-Drug Conjugates (RDCs), leveraging its ability to selectively target CXCR4-expressing cells. Its application is significant in the field of targeted cancer therapies, facilitating precise delivery of therapeutic radionuclides to tumor sites.
  48. Liposome

    DOTA Conjugated JM#21 derivative 7 is a CXCR4-targeting peptide conjugated with DOTA, designed for the synthesis of radioligands. When radiolabeled as 177Lu-DOTA, it demonstrates superior targeting of CXCR4-expressing tumors while exhibiting minimal uptake in non-targeted organs, except for the kidneys. This compound is ideal for research applications involving Radionuclide-Drug Conjugates (RDCs), facilitating advancements in targeted radiotherapy.
  49. LRRK2 Inhibitor

    Lu AF58786 is a selective inhibitor of LRRK2, demonstrating potent activity with an IC50 of 12 nM. It effectively inhibits both the LRRK2 G2019S and LRRK2 A2016T mutations, with IC50 values of 19 nM and 93 nM, respectively. Additionally, Lu AF58786 prevents the phosphorylation of LRRK2, Rab10, and Rab12 in human peripheral blood mononuclear cells. This compound is suitable for research applications focused on Parkinson's disease.
  50. PROTAC LRRK2 Degrader

    PROTAC LRRK2 Degrader-4 is a potent PROTAC designed to target and degrade LRRK2 with a DC50 of 0.79 nM. It exhibits significant biological activity, making it a valuable tool for research into Parkinson's disease and associated inflammatory pathways. This compound enables studies into the modulation of LRRK2 levels, thereby facilitating deeper understanding of its role in neurodegeneration and inflammation.

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