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Autophagy Signaling

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Items 1-50 of 52

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  1. 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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  2. 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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  3. 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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  4. A10603
    Monensin sodium

    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.
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  5. 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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  6. A10698
    Parthenolide ((-)-Parthenolide)

    Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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  7. 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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  8. A10741
    Polydatin (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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  9. A10746
    PP242 (Torkinib)

    mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
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  10. A10765
    Quercetin dihydrate (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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  11. 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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  12. A10845
    Simvastatin

    HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
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  13. A10855
    Valproic acid sodium salt

    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.
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  14. 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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  15. 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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  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. 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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  18. 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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  19. A11151
    3-Methyladenine

    Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
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  20. 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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  21. 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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  22. 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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  23. 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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  24. 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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  25. 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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  26. 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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  27. 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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  28. 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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  29. 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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  30. 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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  31. 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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  32. 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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  33. 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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  34. A14955
    S-Ruxolitinib

    JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
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  35. A15504
    PF-06447475

    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.
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  36. 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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  37. A16358
    Lys05 (Lys01 free base)

    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.
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  38. A17125
    CZC-25146

    LRRK2 inhibitor

    CZC-25146 is a potent LRRK2 inhibitor.
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  39. 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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  40. 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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  41. 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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  42. A17744
    atorvastatin

    CoA reductase inhibitor

    Atorvastatin, (+/-)- is a Hydroxymethylglutaryl-CoA reductase inhibitor.
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  43. 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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  44. A19668
    CA-5f

    macroautophagy/autophagy inhibitor

    CA-5f is a potent late-stage macroautophagy/autophagy inhibitor via inhibiting autophagosome-lysosome fusion.
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  45. A20192
    IITZ-01

    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.
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  46. A20760
    STO-609

    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.
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  47. A21650
    MRT68921 dihydrochloride

    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.
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  48. A21702
    Lys01 trihydrochloride

    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.
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  49. A22219
    SX-682

    allosteric inhibitor of CXCR1 and CXCR2

    SX-682 is an orally bioavailable, potent allosteric inhibitor of CXCR1 and CXCR2.
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  50. A22404
    Liensinine

    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.
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