Autophagy Signaling

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  1. CXCR4 Antagonist

    ICT5040 is a small molecule antagonist targeting the chemokine receptor CXCR4, with an IC50 of 3.8 μM. This compound effectively inhibits CXCL12-mediated cell proliferation and migration in glioma cells, specifically U87 cells, and suppresses CXCL12-induced intracellular calcium mobilization. ICT5040 serves as a valuable tool for investigating the role of the CXCR4/CXCL12 axis in cancer research and potential therapeutic applications.
  2. CXCR

    CX4338 is a selective inhibitor of the chemokine receptor CXCR2, targeting CXCL8-mediated pathways. This compound effectively inhibits CXCR2-mediated cell migration by suppressing β-arrestin-2 recruitment and receptor internalization while enhancing MAPK activation. CX4338 demonstrates potent inhibition of CXCL8-induced chemotaxis in CXCR2-overexpressing cells and human neutrophils. In vivo studies have shown that CX4338 significantly reduces LPS-induced neutrophil infiltration in mouse bronchoalveolar lavage fluid, highlighting its potential for research in inflammatory and immune responses.
  3. CXCR4 Inhibitor

    TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression.
  4. CXCR4 Antagonist

    CXCR4 antagonist 6 is a potent inhibitor of the CXCR4 receptor, displaying an IC50 value of 79 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, thereby significantly reducing CXCL12/CXCR4-mediated cell migration. Additionally, CXCR4 antagonist 6 demonstrates substantial efficacy in in vivo cancer metastasis models, making it a valuable tool for research in cancer biology and therapeutic development.
  5. CXCR Antagonist

    CXCR4 Antagonist 2 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 47 nM. This compound effectively inhibits CXCR4-mediated signaling, making it a valuable tool for studying its role in various biological processes, including cancer metastasis, immune cell trafficking, and HIV infection. Its selective properties make it suitable for research applications aimed at understanding CXCR4 functions and developing therapeutic strategies targeting this receptor.
  6. CXCR4 Antagonist

    KRH-1636 is a potent CXCR4 antagonist, primarily targeting the CXCR4 receptor. This compound plays a significant role in HIV-1 research by inhibiting the interaction between the virus and the CXCR4 receptor, which is crucial for viral entry into host cells. KRH-1636 serves as a valuable tool for studying the mechanisms of HIV-1 infection and for exploring therapeutic strategies aimed at disrupting CXCR4-mediated pathways.
  7. GPR35/CXCR8 agonist

    GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
  8. Avermectin B1 (Abamectin) is a widely used insecticide and anthelmintic.
  9. CXCR4 antagonist

    WZ811 is a C-X-C chemokine receptor type 4 (CXCR4) antagonist (EC50 = 0.3 nM). Inhibits CXCR4/stromal cell-derived factor-1 (SDF-1)-mediated modulation of cAMP in vitro (EC50 = 1.2 nM).
  10. CXCR4 Inhibitor

    MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration.
  11. autophagin-1 inhibitor

    FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
  12. Mitochondrial respiratory chain inhibitor

    Sulfosuccinimidyl oleate (Sulfo-N-succinimidyl oleate) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate is a potent and irreversible inhibitor of mitochondrial respiratory chain.
  13. CXCR2 antagonists

    CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
  14. LRRK2 kinase inhibitor

    GSK2578215A is a potent leucine-rich repeat kinase 2 (LRRK2) inhibitor (IC50 values are 8.9 and 10.1 nM respectively for LRRK2[G2019S] mutant and wild-type LRRK2 respectively).
  15. LRRK2 Inhibitor III

    HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2.
  16. 15-LO inhibitor

    PD146176 (NSC168807) is a 15-Lipoxygenase (15-LO) inhibitor, which inhibits rabbit reticulocyte 15-LO with a Ki of 197 nM. PD146176 (NSC168807) has a dramatic effect in reducing atherogenesis.
  17. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  18. K+/Na+/Ca+ Channel Blocker

    Dronedarone Hydrochloride is a non-iodinated amiodarone derivative that inhibits Na+, K+ and Ca2+ currents.
  19. JAK1/2 inhibitor

    Ruxolitinib sulfate (INCB018424 sulfate) is the first potent, selective JAK1/2 inhibitor to enter the clinic with IC50s of 3.3 nM/2.8 nM, and has > 130-fold selectivity for JAK1/2 versus JAK3.
  20. LRRK2 inhibitor

    LRRK2-IN-1 inhibits both G2019S mutant and wild-type LRRK2 kinase activity with IC50 values of 6 and 13 nM respectively.
  21. JAK inhibitor

    Ruxolitinib Phosphate is the phosphate salt form of ruxolitinib, an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.
  22. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  23. autophagy inducer

    Flubendazole is an anthelmintic used for protection against internal parasites and worms in dogs and cats.
  24. COX-1/COX-2 inhibitor

    Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
  25. Amiodarone hydrochloride is an antiarrhythmic drug for inhibition of ATP-sensitive potassium channel with IC50 of 19.1 μM.
  26. neuromuscular blocking agent

    Cisatracurium besylate (51W89) is a nondepolarizing neuromuscular blocking agent, antagonizing the action of acetylcholine by inhibiting neuromuscular transmission.
  27. TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.
  28. Betulinic acid is a naturally occurring pentacyclic triterpenoid which has antiretroviral, antimalarial, and anti-inflammatory properties.
  29. Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)
  30. Scutellarin, a main active ingredient extracted from Erigeron breviscapus (Vant.) Hand-Mazz, has been wildly used to treat acute cerebral infarction and paralysis induced by cerebrovascular diseases.
  31. ATG4B inhibitor

    S130 is a high affinity, selective inhibitor of ATG4B (a major cysteine protease) with an IC50 of 3.24 ?M. S130 suppresses autophagy flux.
  32. autophagy (CMA) activator

    QX77 is a chaperone-mediated autophagy (CMA) activator.
  33. LRRK2 inhibitor

    CZC-25146 is a potent and selective LRRK2 inhibitor. CZC-25146 prevents mutant LRRK2-induced injury of cultured rodent and human neurons with mid-nanomolar potency.
  34. cell cycle inhibitor

    Briciclib disodium salt is a benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity.
  35. LRRK2 inhibitor

    GNE-7915 is a Blood-Brain Barrier (BBB) penetrable small molecule inhibitor of Leucine-Rich Repeat Kinase 2 (LRRK2).
  36. HMG-CoA reductase inhibitor

    Pitavastatin Lactone is an HMG-CoA reductase inhibitor.
  37. LRRK2 inhibitor

    GNE-0877 is a highly potent and selective LRRK2 inhibitor.
  38. CXCR2 antagonist

    SB 265610 is a nonpeptide, allosteric, inverse agonist of CXCR2 (Kd = 2.51 nM) that prevents receptor activation by binding to a region distinct from the agonist binding site. It does not bind to the related CXCR1 receptor.1 It has been shown to prevent neutrophil chemotaxis both in vitro and in a rat model of hyperoxia-induced lung injury.
  39. Hydroxychloroquine Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
  40. CXCR2 antagonist

    SB225002 is a potent, and selective CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, > 150-fold selectivity over the other 7-TMRs tested.
  41. CCR1 antagonist

    BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1), exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
  42. Autophagy inhibitor

    ROC-325 is an autophagy inhibitor. ROC-325 exhibited superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in 12 different cancer cell lines with diverse genetic backgrounds.
  43. glucocorticoid receptor agonist

    Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone.
  44. ATG4B antagonist

    NSC 185058 is an inhibitor of ATG4B, a cysteine protease that activates LC3B during the initiation of autophagy.
  45. LRRK2 inhibitor

    CZC-25146 is a potent LRRK2 inhibitor.
  46. CXCR4 Antagonist

    MSX-130 is CXCR4 antagonist.
  47. CXCR4 receptor modulator

    NSC-23026 is a CXCR4 receptor modulator.
  48. LRRK2 inhibitor

    PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.
  49. PPT1 inhibitor

    DC661 is a potent palmitoyl-protein thioesterase 1 (PPT1) inhibitor. DC661 inhibits autophagy. DC661 is capable of deacidifying the lysosome and inhibiting autophagy significantly better than hydroxychloroquine (HCQ).
  50. Autophagy inhibitor

    Autophinib is a novel potent autophagy inhibitor, inhibiting autophagy induced by starvation or Rapamycin by targeting the lipid kinase VPS34.

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