Autophagy Signaling

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  1. LRRK2 PROTAC Degrader

    PROTAC LRRK2 Degrader-1 is a targeted protein degrader that selectively engages leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 value of less than 10 nM. This compound is designed for the study of LRRK2-mediated pathways and offers significant potential for advancing research on Parkinson's disease. Its ability to induce targeted degradation makes it a valuable tool for investigating therapeutic strategies in neurodegenerative disorders associated with LRRK2 dysregulation.
  2. LRRK2 PROTAC Degarder

    JH-XII-03-02 is a potent and selective LRRK2 PROTAC degrader. It induces targeted degradation of LRRK2 protein, making it a valuable tool for investigating the role of LRRK2 in Parkinson's disease. This compound is suitable for research applications focused on elucidating LRRK2 function and exploring therapeutic strategies for neurodegenerative disorders.
  3. LRRK2 Inhibitor

    EB-42486 is a potent and highly selective inhibitor of the G2019S mutant variant of LRRK2, exhibiting an IC50 of less than 0.2 nM. This compound demonstrates significant biological activity in cellular models, making it a valuable tool for investigating the role of LRRK2 in Parkinson's disease. Researchers can utilize EB-42486 to explore potential therapeutic strategies aimed at modulating LRRK2 activity in neurodegenerative disorders.
  4. LRRK2 Kinase Inhibitor

    LRRK2-IN-7 is a potent and selective inhibitor of the LRRK2 kinase, exhibiting an IC50 of 0.9 nM. This compound demonstrates over 1000-fold selectivity against other kinases, ion channels, and cytochrome P450 enzymes. Due to its ability to penetrate the central nervous system (CNS), LRRK2-IN-7 is valuable for studies related to neurodegenerative diseases and the physiological roles of LRRK2 in cellular signaling pathways.
  5. LRRK2 Inhibitor

    MK-1468 is a selective LRRK2 inhibitor known for its oral bioavailability and ability to cross the blood-brain barrier. This compound has demonstrated significant potential in studying the pathophysiology of Parkinson's disease, making it a valuable tool for researchers investigating therapeutic mechanisms and interventions in neurodegenerative disorders related to LRRK2 activity.
  6. LRRK2 Inhibitor

    GNE-7915 tosylate is a potent and selective inhibitor of LRRK2, exhibiting an IC50 of 9 nM. This compound demonstrates effective brain penetration, making it a valuable tool for studying LRRK2-related pathways in neurological diseases. Its specificity allows for targeted research into the role of LRRK2 in conditions such as Parkinson's disease and other neurodegenerative disorders.
  7. LRRK2 Inhibitor

    LRRK2-IN-2 is a potent and selective inhibitor of the Leucine-rich repeat kinase 2 (LRRK2) with an IC50 of less than 0.6 nM. This orally active compound demonstrates excellent brain penetration, making it valuable for studies focused on Parkinson’s disease. Its specificity and efficacy support a range of neurobiological research applications related to LRRK2's role in neurodegeneration.
  8. LRRK2 Inhibitor

    LRRK2-IN-3 is a potent and selective inhibitor of LRRK2, exhibiting an IC50 of 2.6 nM in human peripheral blood mononuclear cells (PBMCs). This orally active compound demonstrates effective brain penetration, making it an invaluable tool for studying LRRK2's role in neurodegenerative disorders. Its application in Parkinson's disease research allows for deeper insights into disease mechanisms and therapeutic strategies targeting LRRK2 pathways.
  9. LRRK2 Inhibitor

    LRRK2-IN-16 is a selective inhibitor of the LRRK2 kinase with an IC50 value of less than 5 μM. This compound is valuable for investigating neurodegenerative and autoimmune disorders, providing insights into the role of LRRK2 in these pathologies. Its use in research can enhance understanding of disease mechanisms and aid in the development of therapeutic strategies targeting LRRK2.
  10. G2019S-LRRK2 Kinase Inhibitor

    LRRK2-IN-10 is a potent and mutation-selective inhibitor targeting the G2019S variant of LRRK2 kinase. It exhibits IC50 values of 11 nM and 5.2 nM for phosphorylated sites pS935 and pS1292, respectively, demonstrating its effectiveness in modulating LRRK2 activity. This compound is particularly valuable for research related to Parkinson’s disease, offering insights into the mechanisms of G2019S-LRRK2 in neurological contexts.
  11. LRRK2 Inhibitor

    CZC-54252 hydrochloride is a potent and selective inhibitor of LRRK2, exhibiting IC50 values of 1.28 nM for wild-type and 1.85 nM for the G2019S mutant variant. This compound effectively attenuates G2019S LRRK2-induced neuronal injury, with an EC50 of approximately 1 nM, showcasing its neuroprotective properties. CZC-54252 hydrochloride is valuable for research applications focused on neurodegenerative diseases associated with LRRK2 modulation.
  12. LRRK2 Inhibitor

    SRI-31255 is an orally active inhibitor of Leucine-rich repeat kinase 2 (LRRK2), exhibiting IC50 values of 520 nM and 427 nM for human wild-type and G2019S mutant forms, respectively. By binding to the ATP-binding pocket of LRRK2, SRI-31255 effectively inhibits kinase activity, providing neuroprotective effects. This compound is a valuable tool for research aimed at developing LRRK2-targeted therapies for Parkinson's disease.
  13. LRRK2 Inhibitor

    LRRK2-IN-14 is a potent LRRK2 inhibitor with a remarkable IC50 of 6.3 nM specifically targeting the LRRK2(G2019S) mutation. This compound exhibits significant inhibitory activity against hERG with an IC50 of 22 μM. Notably, LRRK2-IN-14 demonstrates permeability across the blood-brain barrier, making it a valuable tool for studying neurodegenerative diseases related to LRRK2 dysregulation. Its pharmacological profile positions it as a promising candidate for research applications in Parkinson's disease and other related disorders.
  14. LRRK2 Inhibitor

    LRRK2-IN-6 is a selective inhibitor of leucine-rich repeat kinase 2 (LRRK2) with potent activity demonstrated by IC50 values of 4.6 μM for GS LRRK2 and 49 μM for wild-type LRRK2. This compound effectively inhibits autophosphorylation at Ser1292 and Ser925, key sites associated with LRRK2 activity. LRRK2-IN-6's ability to cross the blood-brain barrier makes it a valuable tool for research in neurodegenerative diseases linked to LRRK2 dysregulation.
  15. LRRK2 Inhibitor

    SRI-29132 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2). It exhibits significant activity in modulating LRRK2-related pathways, making it a valuable tool for investigating the pathophysiology of Parkinson's disease and the development of potential therapeutic strategies. Research utilizing SRI-29132 can provide insights into the role of LRRK2 in neurodegenerative processes and neuronal signaling.
  16. PROTAC LRRK2 Degrader

    PROTAC LRRK2 Degrader-3 primarily targets the LRRK2 protein through a PROTAC mechanism, exhibiting a DC50 of 0.17 nM. This compound effectively promotes the degradation of LRRK2, making it a valuable tool for research in Parkinson’s disease and inflammation. Its unique structure comprises a specific LRRK2 ligand, a Cereblon ligand, and an optimized linker, facilitating targeted therapeutic investigations.
  17. LRRK2 Inhibitor

    LRRK2-IN-20 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), exhibiting a pIC50 of 0.7921 nM. This compound is primarily utilized in the study of Parkinson's disease, enabling researchers to explore LRRK2's role in disease pathology and therapeutic interventions. Its potent inhibition provides a valuable tool for investigating the underlying mechanisms of neurodegeneration and potential treatment strategies.
  18. LRRK2 Inhibitor

    LRRK2-IN-4 is a potent and selective inhibitor of leucine-rich repeat kinase 2 (LRRK2), exhibiting an IC50 of 2.6 nM. This compound demonstrates good central nervous system penetration and oral bioavailability, making it a valuable tool for studying LRRK2's role in cellular signaling. LRRK2-IN-4 is particularly relevant for research into Parkinson’s disease, providing a means to explore therapeutic strategies targeting this kinase in related pathophysiological contexts.
  19. LRRK2 Inhibitor

    PF-06455943 is a potent inhibitor of leucine-rich repeat kinase 2 (LRRK2) with an IC50 of 3 nM. This compound also functions as a PET radioligand, making it valuable for imaging studies. PF-06455943 is primarily utilized in research investigating ADME/neuro pharmacokinetics and offers insights into pathophysiological mechanisms associated with Parkinson's disease (PD).
  20. LRRK2 Inhibitor

    LRRK2-IN-5 is a selective inhibitor of the leucine-rich repeat kinase 2 (LRRK2), demonstrating potent inhibitory activity with IC50 values of 1.2 μM for GS LRRK2 and 16 μM for wild-type LRRK2. This compound effectively inhibits LRRK2 autophosphorylation at the Ser1292 and Ser925 sites, making it a valuable tool for studying LRRK2's role in various neurological disorders. Additionally, LRRK2-IN-5 is capable of crossing the blood-brain barrier, facilitating its application in central nervous system research.
  21. LRRK2 Kinase Inhibitor

    (R,R)-LRRK2-IN-7 is a selective LRRK2 kinase inhibitor, exhibiting a potent inhibitory activity with an IC50 of 0.9 nM. This compound demonstrates over 1000-fold selectivity against various other kinases, ion channels, and CYP enzymes, making it a valuable tool for studies involving LRRK2-associated pathologies. Its ability to penetrate the central nervous system (CNS) enhances its relevance for research applications in neurodegenerative diseases.
  22. LRRK2 PROTAC Degrader

    ROTAC LRRK2 degrader-1 is a potent PROTAC degrader targeting LRRK2, a protein associated with neurodegenerative diseases. This compound facilitates the targeted degradation of LRRK2, which is implicated in the pathogenesis of Parkinson’s Disease. ROTAC LRRK2 degrader-1 can be utilized in research to investigate LRRK2-related biological pathways and therapeutic interventions for Parkinson’s Disease and other associated disorders.
  23. LRRK2 Inhibitor

    LY2023-001 is a selective inhibitor of the G2019S mutation in LRRK2, exhibiting a potent inhibitory activity with an IC50 of 12.9 nM. This compound interacts with critical residues, forming stable hydrogen bonds with Glu1948 and Ala1950 in the G2019S LRRK2 protein. It serves as a valuable tool for investigating the role of LRRK2 signaling in neurodegenerative disorders, facilitating research in cellular models and drug development for Parkinson's disease.
  24. LRRK2 Inhibitor

    LRRK2-IN-12 is a potent inhibitor of LRRK2, effectively targeting G2019S (IC50=0.45 nM) and wild-type LRRK2 (IC50=1.1 nM), with a similar affinity for the wild-type enzyme in the presence of ADP (IC50=0.46 nM). This compound is valuable for research into neurodegenerative diseases, particularly in investigating the role of LRRK2 in Alzheimer's Disease. Its high specificity and low nanomolar activity make it an essential tool for exploring LRRK2-related pathways and therapeutic interventions.
  25. LRRK2 PROTAC Degrader

    PROTAC LRRK2 Degrader-2 is designed to target LRRK2 through a PROTAC mechanism, exhibiting a DC50 of 0.14 nM. This compound effectively recruits LRRK2 or its mutants to the cereblon E3 ubiquitin ligase, facilitating targeted ubiquitination and subsequent proteasomal degradation of LRRK2. It serves as a valuable tool for research focused on Parkinson's disease and the study of LRRK2-related pathways.
  26. Mitochondria Targeting AUTAC

    AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC) designed to downregulate cytosolic proteins while promoting selective mitochondrial degradation through mitophagy. This compound is valuable in studying the mechanisms of mitophagy and its implications in mitochondrial health and disease. It holds potential for applications in research focusing on mitochondrial dysfunction and the role of autophagy in cellular homeostasis.
  27. mitochondrial autophagy

    T-271 is a selective inducer of mitochondrial autophagy, specifically targeting the regulation of mitophagy processes within cells. This compound facilitates the degradation and removal of damaged mitochondria, promoting cellular homeostasis and contributing to mitochondrial quality control. T-271 is primarily utilized in research focused on metabolic disorders, neurodegeneration, and other conditions associated with mitochondrial dysfunction.
  28. ULK1-Recruiting Chimeras

    NZ-66 is a chimera that targets UNC-51-like kinase 1 (ULK1), facilitating proximity-induced degradation of mitochondria through ULK1 activation. This compound effectively induces mitophagy, making it a valuable tool for studying mitochondrial quality control processes. Additionally, NZ-66 holds potential in research related to neurodegenerative disorders, offering insights into therapeutic strategies for these conditions.
  29. Autophagy Inhibitor

    Leonurine hydrochloride is an alkaloid derived from Leonurus artemisia, acting primarily as an autophagy inhibitor. This compound exhibits notable anti-oxidative and anti-inflammatory properties, making it a valuable tool for research into cellular stress responses and inflammatory processes. It is particularly useful for studying the implications of autophagy modulation in various biological contexts, including neurodegenerative diseases and cancer.
  30. Ivermectin is a broad-spectrum antiparasitic avermectin medicine.
  31. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  32. autophagy inhibitor

    Monensin sodium is an ionophore and inhibitor of autophagy commercially used in livestock feed. It inhibits autophagy, interfering with the fusion of the autophagosome and the lysosome.
  33. Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
  34. Pyrazinamide is an antimycobacterial compound that inhibits the growth of the human M. tuberculosis H37Rv strain.
  35. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  36. Salidroside (Rhodioloside) is a glucoside of tyrosol found in the plant Rhodiola rosea. It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin.
  37. HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  38. HDAC inhibitor

    Valproic acid sodium salt (Sodium Valproate) is an 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.
  39. Autophagy Inducer

    STF-62247 is a small molecule agonist that induces autophagy and selectively causes lethality in renal cell carcinoma (RCC) cells that have lost the von Hippel-Lindau (VHL) tumor suppressor activity (IC50 = 625 nM).
  40. CXCR2 ligand

    SRT3109 is a CXCR2 ligand for use in the treatment of chemokine mediated diseases and conditions.
  41. CXCR4 agonist

    CTCE-0214 is a chemokine CXC receptor 4 (CXCR4) agonist, SDF-1α (stromal cell-derived factor-1α) peptide analog. CTCE-0214 shows anti-inflammatory activity, and can be used in inflammation sepsis and systemic inflammatory syndromes research.
  42. Antileukinate, a hexapeptide, is a potent inhibitor of CXC-chemokine receptor (CXCR). Antileukinate inhibits neutrophil chemotaxis and activation. Antileukinate can be used for the research of acute inflammation and injury.
  43. Calcium channel antagonist

    Felodipine is a 1,4-dihydropyridine antagonist and calcium channel protein inhibitor.

  44. PI3K activator

    740 Y-P (740YPDGFR; PDGFR 740Y-P) is a potent and cell-permeable PI3K activator. 740 Y-P readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone.
  45. CTCE-9908 is a potent and selective CXCR4 antagonist. CTCE-9908 induces mitotic catastrophe, cytotoxicity and inhibits migration in CXCR4-expressing ovarian cancer cells.
  46. HMGB1 release inhibitor

    Ethyl pyruvate is a simple derivative of the endogenous metabolite, pyruvic acid. Ethyl pyruvate is an anti-inflammatory agent.
  47. autophagy inhibitor

    EAD1 is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 also induces apoptosis.
  48. LRRK2 inhibitor

    PF-06454589 is a potent and selective LRRK2 inhibitor.
  49. anti-infective agent

    Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities.
  50. ATG4 Autophagy Related 4 Homolog B Human Recombinant

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