Autophagy Signaling

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  1. Autophagy Inhibitor

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

  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. lysosomal exocytosis inhibitor

    Vacuolin-1 is a potent and cell-permeable lysosomal exocytosis inhibitor.
  7. 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.
  8. allosteric inhibitor of CXCR1 and CXCR2

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

    VPS34 inhibitor 1 (Compound 19, PIK-III analogue) is a potent and selective inhibitor of VPS34 with an IC50 of 15 nM.
  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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.
  16. retinoic acid metabolism inhibitor

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

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

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

    LRRK2 inhibitor 1 is a potent, selective and oral LRRK2 inhibitor with an pIC50 of 6.8 nM.
  20. 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.
  21. LRRK2 inhibitor

    PFE-360, also known asd PF-06685360, is a potent and selective inhibitor of LRRK2 kinase.
  22. 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.
  23. 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.
  24. Cholesterol biosynthesis inhibitor

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

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. CXCR4/STAT3 Inhibitor

    Minecoside is a potent inhibitor of the CXCR4 receptor and STAT3 signaling pathway. It demonstrates significant anticancer and anti-inflammatory activities by downregulating CXCR4 expression and suppressing STAT3 activation, which leads to the inhibition of CXCL12-induced cellular invasion. Minecoside has been shown to effectively hinder cancer metastasis and enhance apoptosis, making it a valuable tool for research in cancer biology and therapeutic development.
  44. Cathepsin Inhibitor

    LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways.
  45. Autophagy Inhibitor/Purinergic Receptors Antagonist

    Indophagolin is a potent autophagy inhibitor targeting purinergic receptors, demonstrating an IC50 of 140 nM. It effectively antagonizes the P2X4, P2X1, and P2X3 receptors with IC50 values of 2.71, 2.40, and 3.49 μM, respectively. Additionally, Indophagolin inhibits Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors, with IC50s ranging from 3.4 to 15.4 μM. It exhibits strong antagonistic effects on the serotonin receptor 5-HT6 (IC50=1.0 μM) and moderate effects on multiple serotonin receptors, making it a valuable tool for research into autophagy and neurological pathways.
  46. Autophagy Inhibitor

    Autogramin-1 is a potent autophagy inhibitor that effectively suppresses autophagic processes triggered by nutrient deprivation or mTORC1 inhibition. With an IC50 of 0.17 μM against starvation-induced autophagy and 0.44 μM against Rapamycin-induced autophagy, it serves as a valuable tool for researching the role of autophagy in cellular processes and disease models. This compound provides insights into autophagic regulation and its implications in various cancer and neurodegenerative studies.
  47. Autophagy Inhibitor

    NEO214 is an autophagy inhibitor that acts by preventing autophagy-lysosome fusion, effectively blocking autophagic flux. This compound, a covalent conjugate of the PDE4 inhibitor Rolipram and perillyl alcohol, exhibits anti-cancer activity and is capable of penetrating the blood-brain barrier. Its mechanism involves the activation of mTOR and aggregation of the transcription factor EB (TFEB), promoting the death of glioma cells. NEO214 may provide a strategy to combat chemotherapy resistance in glioblastoma.
  48. Atg4B Inhibitor

    Atg4B-IN-2 is a selective inhibitor of Atg4B with a competitive mechanism, exhibiting a Ki value of 3.1 μM. In addition, it displays moderate inhibitory activity against phospholipase A2, with IC50 values of 11 μM and 3.5 μM for Atg4B and PLA2, respectively. This compound effectively enhances the anticancer efficacy of agents targeting castration-resistant prostate cancer through the inhibition of autophagy, making it a valuable tool for cancer research.
  49. Autophagy Inhibitor

    CUR5g is a selective autophagy inhibitor that targets the fusion of autophagosomes and lysosomes. By inhibiting the recruitment of STX17 to autophagosomes through a UVRAG-dependent mechanism, CUR5g effectively disrupts the degradation of autophagic substrates in cancer cells. This compound enhances the anticancer efficacy of Cisplatin in both in vitro and in vivo models, making it a valuable tool for studying autophagy's role in cancer treatment and potential therapeutic synergies.
  50. 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.

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