Autophagy Signaling

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  1. PARP inhibitor

    Olaparib (AZD2281) is an inhibitor of poly ADP ribose polymerase (PARP), an enzyme involved in DNA repair.
  2. 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).
  3. 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.
  4. 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.
  5. 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).
  6. Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
  7. 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.
  8. 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.
  9. mTOR Inhibitor

    PP242 is a potent and selective mTOR inhibitor in both mTORC1 and mTORC2.
  10. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  11. MAO-B inhibitor

    Quercetin inhibits many enzyme systems including tyrosine protein kinase, phospholipase A2, phosphodiesterases, mitochondrial ATPase, PI 3-kinase and protein kinase C.
  12. HMG-CoA reductase inhibitor

    Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.
  13. 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.
  14. 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).
  15. MEK inhibitor

    U0126-EtOH is an inhibitor of both MEK1 and MEK2 with an IC50 of 72 nM and 58 nM respectively.
  16. HDAC inhibitor

    Vorinostat is an inhibitor of HDACs, inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors.
  17. 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;
  18. 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.
  19. Autophagy/PI3K Inhibitor

    3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).
  20. Protein translocation Inhibitor

    Brefeldin A blocks binding of ADP-ribosylation factor to the Golgi apparatus and inhibits GDP-GTP exchange.
  21. 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.
  22. LRRK2 inhibitor

    LRRK2-IN-1 inhibits both G2019S mutant and wild-type LRRK2 kinase activity with IC50 values of 6 and 13 nM respectively.
  23. 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.
  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. 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).
  26. 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.
  27. autophagin-1 inhibitor

    FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
  28. 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.
  29. 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).
  30. LRRK2 Inhibitor III

    HG-10-102-01 is a brain penetrant, potent and selective inhibitor of wild-type LRRK2.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. LRRK2 inhibitor

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

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

    GNE-0877 is a highly potent and selective LRRK2 inhibitor.
  39. 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.
  40. 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.
  41. 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.

  42. Topoisomerase II inhibitor

    Doxorubicin is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.
  43. JAK inhibitor

    S-Ruxolitinib is the chirality of INCB018424, is a potent and selective small-molecule Janus kinase 1 (JAK1) and JAK2 inhibitor.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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 .
  49. Autophagy Inhibitor

    PIK-III is a selective inhibitor of ?VPS34 enzymatic activity.
  50. 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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