Autophagy Signaling

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. LRRK2 inhibitor

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

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

    GNE-0877 is a highly potent and selective LRRK2 inhibitor.
  8. 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.
  9. LRRK2 inhibitor

    CZC-25146 is a potent LRRK2 inhibitor.
  10. LRRK2 inhibitor

    PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.
  11. 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).
  12. Autophagy inhibitor

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

    Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor.
  14. LRRK2 inhibitor

    JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor, with IC50 of 6.6 nM, 2.2 nM ,47.7 nM for LRRK2-wild-type, LRRK2-G2019S, LRRK2-A2016T.
  15. EGFR inhibitor

    Olafertinib (CK-101, RX518) is an epidermal growth factor receptor (EGFR) inhibitor.

     
  16. Autophagy Inhibitor

    Vps34-PIK-III (PIK-III) is a selective inhibitor of VPS34 enzymatic activity.

  17. Autophagy inhibitor

    Lys05 is a potent lysosomal autophagy inhibitor. Lys05 is a previously undescribed dimeric chloroquine which more potently accumulates in the lysosome and blocks autophagy compared with HCQ.
  18. ULK1/ULK2 inhibitor

    MRT68921 dihydrochloride is the most potent inhibitor of ULK1 and ULK2, with IC50 values of 2.9 nM and 1.1 nM, respectively.
  19. lysosomal autophagy inhibitor

    Lys01 trihydrochloride (Lys05) is a novel lysosomal autophagy inhibitor with IC50 values of 3.6, 3.8, 6 and 7.9 μM for 1205Lu, c8161, LN229 and HT-29 cell line in the MTT assay.
  20. dual ULK1/ULK2 autophagy inhibitor

    SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively.
  21. lysosomal exocytosis inhibitor

    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor.
  22. inhibitor of quinone reductase 2 (QR2)

    S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1.
  23. allosteric inhibitor of CXCR1 and CXCR2

    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.
  24. VPS34 inhibitor

    VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
  25. autophagy/mitophagy inhibitor

    Liensinine is an autophagy/mitophagy inhibitor. Liensinine, a major isoquinoline alkaloid, extracted from the seed embryo of Nelumbo nucifera Gaertn, has a wide range of biological activities, including anti-arrhythmias, anti-hypertension, anti-pulmonary fibrosis, relaxation on vascular smooth muscle, etc.
  26. late-stage autophagy inhibitor

    PHY34 is a late-stage autophagy inhibitor with nanomolar potency and significant antitumor efficacy as a single agent against HGSOC in vivo.
  27. brain penetrant LRRK2 inhibitor

    MLi-2 is a potent, highly selective, orally available, brain penetrant inhibitor of LRRK2 with an IC50 of 0.76 nM.
  28. p110β inhibitor

    Rac)-AZD 6482 ((Rac)-KIN-193) is a less active racemate of AZD 6482. AZD 6482 is a potent and selective p110β inhibitor with an IC50 of 0.69 nM.
  29. CaM-KK inhibitor

    STO-609 is a selective and cell-permeable inhibitor of the Ca2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively.
  30. CYP26 inhibitor/RAMBA

    Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
  31. retinoic acid metabolism inhibitor

    (+)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  32. retinoic acid metabolism inhibitor

    (-)-Talarozole is a potent inhibitor of retinoic acid metabolism extracted from patent WO 1997049704 A1.
  33. macroautophagy/autophagy inhibitor

    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
  34. LRRK2 inhibitor

    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8 nM.
  35. Lysosomotropic autophagy inhibitor

    IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ.
  36. LRRK2 inhibitor

    PFE-360, also known asd PF-06685360, is a potent and selective inhibitor of LRRK2 kinase.
  37. Autophagy inhibitor

    Aumitin is an autophagy inhibitor, targeting mitochondrial complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
  38. Autophagy inhibitor

    EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion.
  39. Cholesterol biosynthesis inhibitor

    Monacolin J is an inhibitor of cholesterol biosynthesis, and inhibits the activity of HMG-CoA reductase.
  40. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  41. CXCL8 receptor inhibitor

    Reparixin L-lysine salt is an inhibitor of CXCL8 receptor, also inhibit CXCR1 and CXCR2 activation,which has been shown to attenuate inflammatory responses in various injury models.
  42. EGFR inhibitor

    AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively.
  43. LRRK2 inhibitor

    PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC50 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively.
  44. LRRK2 inhibitor

    CZC-54252 is a potent inhibitor of LRRK2 with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2 respectively.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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