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  • Autophagy Signaling

Autophagy Signaling

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Items 1-50 of 190

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  1. A10373
    Etoposide (VP-16)

    Topoisomerase II inhibitor

    Etoposide forms a ternary complex with DNA and the topoisomerase II enzyme (which aids in DNA unwinding), prevents re-ligation of the DNA strands, and by doing so causes DNA strands to break. Therefore, this causes errors in DNA synthesis and promotes apoptosis of the cancer cell.
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  2. A14396
    Telaglenastat (CB-839)

    Glutaminase inhibitor

    CB-839 an is orally bioavailable inhibitor of glutaminase, with potential antineoplastic activity. CB-839 (Telaglenastat) also inudces autophagy and has antitumor activity.

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  3. A12942
    Spautin-1

    Autophagy Inhibitor

    Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
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  4. A14403
    Doxorubicin

    Topoisomerase II inhibitor

    Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.
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  5. A17323
    Valproic acid

    HDAC inhibitor

    Valproic acid 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; Valproic acid sodium salt is used in the treatment of epilepsy, bipolar disorder and prevention of migraine headaches.
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  6. A10741
    (E/Z)-Polydatin ((E/Z)-Piceid)

    PLA inhibitor

    Polydatin protects cerebral cells from ischemic damages via improvement of microcirculation and inhibition of platelet aggregation. In addition, polydatin inhibits ICAM-1 expression in endothelial cells stimulated by lipopolysaccharide; it also attenuates adhesion between white blood cells and endothelial cells.
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  7. A10957
    U0126-EtOH

    MEK inhibitor

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
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  8. A10255
    ABT-737

    Bcl-2 Inhibitor

    ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).
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  9. A10746
    PP242 (Torkinib)

    mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
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  10. A17858
    Sunitinib

    multi-targeted receptor tyrosine kinase inhibitor

    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively.
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  11. A11041
    INCB018424 (Ruxolitinib)

    JAK1/2 Inhibitor

    INCB018424 is a potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively;
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  12. A11151
    3-Methyladenine

    Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
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  13. A15880
    MRT68921

    Autophagy ULK1/2 inhibitor

    MRT68921 is a potent and dual autophagy kinase ULK1/2 inhibitor with IC50 of 2.9 nM and 1.1 nM, respectively.
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  14. A11052
    Crenolanib (CP-868596)

    PDGFR/FLT3 Inhibitor

    Crenolanib (CP-868596) is an orally bioavailable, selective small molecule inhibitor of the PDGFR tyrosine kinase, inhibiting both PDGFRA and PDGFRB at picomolar concentrations.
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  15. A12383
    Reparixin

    CXCL8/CXCR1/2 Inhibitor

    Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).
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  16. A10979
    Vorinostat (SAHA)

    HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
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  17. A10880
    Sunitinib Malate

    RTK inhibitor

    Sunitinib is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).
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  18. A15795
    SBI-0206965

    ULK1 inhibitor

    SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50 of 108 nM for ULK1 kinase activity and 711 nM for the highly related kinase ULK2 .
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  19. A10766
    Quercetin (Sophoretin)

    MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
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  20. A14316
    Mdivi-1

    DRP1 inhibitor

    Mdivi-1 is a selective cell-permeable inhibitor of mitochondrial division DRP1 (dynamin-related GTPase) and mitochondrial division Dynamin I (Dnm1) with IC50 of 1-10 uM.
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  21. A14149
    GNE 9605

    LRRK2 inhibitor

    GNE-9605 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki and IC50 of 2 nM and 19 nM, respectively.
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  22. A10737
    Pitavastatin calcium (Livalo)

    HMG-CoA reductase inhibitor

    Pitavastatin Calcium is a competitive inhibitor of the enzyme HMGCR (HMG-CoA reductase) results in a reduction in LDL cholesterol synthesis.
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  23. A10662
    TAE684

    ALK Inhibitor

    TAE684 is a inhibitor of ALK and also a potent inhibitor of LRRK2 kinase activity (IC(50) of 7.8nM against wild-type LRRK2, 6.1nM against the G2019S mutant).
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  24. A10111
    Olaparib (AZD2281)

    PARP inhibitor

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
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  25. A11024
    PF-04691502

    PI3K/mTOR Inhibitor

    PF-04691502 is a PI3K/mTOR kinase inhibitor, is also an agent targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in the PI3K/mTOR signaling pathway.
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  26. A12596
    MSX-122

    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.
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  27. A12603
    FMK 9a

    autophagin-1 inhibitor

    FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
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  28. A12606
    Sulfosuccinimidyl oleate

    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.
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  29. A12798
    GSK2578215A

    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).
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  30. A12919
    HG-10-102-01

    LRRK2 Inhibitor III

    HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2.
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  31. A13347
    PD146176 (NSC168807)

    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.
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  32. A11156
    Brefeldin A

    Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
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  33. A11467
    Ruxolitinib sulfate

    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.
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  34. A11477
    LRRK2-IN-1

    LRRK2 inhibitor

    LRRK2-IN-1 inhibits both G2019S mutant and wild-type LRRK2 kinase activity with IC50 values of 6 and 13 nM respectively.
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  35. A11552
    Ruxolitinib Phosphate

    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.
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  36. A11797
    Aspirin

    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.
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  37. A13376
    S130

    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.
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  38. A13448
    CZC-25146 hydrochloride

    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.
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  39. A13649
    Briciclib disodium salt

    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.
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  40. A13748
    GNE-7915

    LRRK2 inhibitor

    GNE-7915 is a Blood-Brain Barrier (BBB) penetrable small molecule inhibitor of Leucine-Rich Repeat Kinase 2 (LRRK2).
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  41. A13896
    Pitavastatin Lactone

    HMG-CoA reductase inhibitor

    Pitavastatin Lactone is an HMG-CoA reductase inhibitor.
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  42. A13969
    GNE0877

    LRRK2 inhibitor

    GNE-0877 is a highly potent and selective LRRK2 inhibitor.
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  43. A17031
    ROC-325

    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.
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  44. A17125
    CZC-25146

    LRRK2 inhibitor

    CZC-25146 is a potent LRRK2 inhibitor.
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  45. A17221
    PF-06371900

    LRRK2 inhibitor

    PF-06371900 is a potent and highly selective leucine rich repeat kinase 2 (LRRK2) inhibitor.
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  46. A17236
    DC661

    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).
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  47. A17241
    Autophinib

    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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  48. A17744
    ent-Atorvastatin

    CoA reductase inhibitor

    Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor.
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  49. A15777
    JH-II-127

    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.
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  50. A15847
    Olafertinib (CK-101, RX518)

    EGFR inhibitor

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

     
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