Metabolism

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  1. Hsp90 inhibitor

    VER-49009 is a pyrazole compound that inhibits Hsp90 with an IC50 value of 47 nM.
  2. ATGL inhibitor

    Atglistatin is a highly potent, selective and competitive inhibitor of adipose triglyceride lipase (ATGL) with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, but no toxicity up to a concentration of 50 μM.
  3. Hsp90 inhibitor

    VER-50589 is an isoxazole compound that inhibits Hsp90 with an IC50 value of 21 nM.
  4. VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
  5. Trx-1 inhibitor

    PX 12 inhibits hypoxia-induced HIF-1a transcriptional activity (IC50 11 nM) and proliferation of HT29 and MCF-7 tumor cells (IC50 1.9 and 0.9 uM, respectively).
  6. NS5B Inhibitor

    ABT333 is an NS5B non-nucleoside polymerase inhibitor.
  7. PLD inhibitor

    Isoforms of phospholipase D (PLD) cleave the head group from phospholipids, releasing the second messenger phosphatidic acid (PA), which can produce changes in Ras activation, cell spreading, stress fiber formation, chemotaxis, and membrane vesicle trafficking. FIPI is a derivative of halopemide which potently inhibits both PLD1 (IC50 = 25 nM) and PLD2 (IC50 = 20 nM).
  8. HMG-CoA reductase inhibitor

    Pitavastatin Lactone is an HMG-CoA reductase inhibitor.
  9. Pim-1 inhibitor

    Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.
  10. HIF-PH inhibitor

    DMOG is a cell permeable, competitive inhibitor of HIF-PH. It acts to stabilize HIF-1α expression at normal oxygen tensions in cultured cells, at concentrations between 0.1 and 1 mM.
  11. 11β-hydroxylase inhibitor

    Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
  12. FTase inhibitor

    LB42708 is a potent, orally active and selective nonpeptidic farnesyltransferase inhibitor (FTase inhibitor).
  13. tryptophan hydroxylase inhibitor

    Telotristat (LP-778902) is a potent tryptophan hydroxylase inhibitor with an in vivo IC50 of 0.028 μM.
  14. NAMPT inhibitor

    STF 118804 is a highly specific NAMPT inhibitor that reduces the viability of most B-ALL cell lines with high potency IC50 values in the low nanomolar range and improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia.
  15. factor Xa inhibitor

    DPC423 is a highly potent and orally bioavailable pyrazole antithrombotic agent.
  16. C75

    FASN inhibitor

    C75 is a novel, potent synthetic inhibitor of fatty acid synthase (FAS), which is used as a tool for studying fatty acid synthesis in metabolic disorders and cancer.
  17. Grp94 Inhibitor

    PU-WS13 is a potent, Grp94-specific Hsp90 inhibitor of the purine scaffold class. PU-WS13 is a cell-permeable inhibitor of Grp94 with EC50 of 220 nM.
  18. XOR Inhibitor

    Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM.
  19. PAI-1 inhbitor

    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
  20. metalloendopeptidase inhibitor

    Phosphoramidon Disodium Salt is a metalloendopeptidase inhibitor.
  21. Lp-PLA2 Inhibitor

    Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor .
  22. HSP90 inhibitor

    CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
  23. PFKFB3 inhibitor

    PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) with IC50 of 207 nM.
  24. HSP90 inhibitor

    NMS-E973 is a potent and selective Hsp90 inhibitor.
  25. Ribonucleotide reductase inhibitor

    Triapine is a potent ribonucleotide reductase inhibitor with broad spectrum antitumor activity by inhibiting DNA synthesis.
  26. Factor Xa inhibitor

    Edoxaban is a selective factor Xa inhibitor with Ki of 0.561 nM
  27. IDO inhibitor

    NLG919 is an orally available inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), with potential immunomodulating and antineoplastic activities.
  28. Tph1 inhibitor

    LP-533401 is a small molecule inhibitor of Tph1.
  29. Phospholipase C inhibitor

    U 73122 is a phospholipase C inhibitor. It inhibits agonist-induced platelet aggregation with IC50 values of 1-5 uM.
  30. MAO inhibitor

    RN-1 2HCl exhibits selectivity for LSD1 over monoamine oxidase (MAO)-A and MAO-B (IC50 values are 70 nM, 0.51 and 2.79 μM respectively, in a horseradish peroxidase-coupled assay).
  31. glucosidase I/II inhibitor

    Deoxynojirimycin is a Maltase-glucoamylase (a-glucosidase I and II) inhibitor. It interferes with N-linked glycosylation.
  32. IDH1 inhibitor

    AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
  33. pan-HSP inhibitor

    KNK437, dose-dependently inhibited the acquisition of thermotolerance and the induction of various HSPs including HSP105, HSP70, and HSP40 in COLO 320DM (human colon carcinoma) cells.
  34. IDO inhibitor

    Indoximod is a methylated tryptophan with anti-immunosuppressive activity.
  35. PFK-2/FBPase inhibitor

    PFK-158 is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) and derivative of 3-(3-pyridinyl)-1-[4-pyridinyl]-2-propen-1-one (3PO), with potential antineoplastic activity.
  36. FLAP inhibitor

    AZD6642 is an inhibitor of 5-Lipoxygenase Activating Protein (FLAP) for the treatment of inflammatory diseases.
  37. CAIX inhibitor/ radiosensitizer

    DTP348 is an oral dual CAIX inhibitor/ radiosensitizer.
  38. FTase Inhibitor

    FTI-277 HCl is an inhibitor of farnesyl transferase (FTase); a highly potent Ras CAAX peptidomimetic which antagonizes both H- and K-Ras oncogenic signaling.
  39. 5-lipoxygenase inhibitor

    Esculetin, a phenolic compound, acts as a 5-LO (5-lipoxygenase, 5-LOX) inhibitor.
  40. alpha-glucosidase inhibitor

    Voglibose is an N-substituted derivative of valiolamine, excellent inhibitory activity against alpha-glucosidases and its action against hyperglycemia and various disorders caused by hyperglycemia.
  41. Carbonic anhydrase (CA) inhibitor

    U-104 is a novel ureido-sulfonamide inhibitor of Carbonic Anhydrase IX (CAIX).
  42. Factor Xa inhibitor

    5-R-Rivaroxaban is (R) enantiomer of Rivaroxaban. Rivaroxaban is a novel, oral, direct Factor Xa (FXa) inhibitor in late-stage development for the prevention and treatment of thromboembolic disorders.
  43. DGAT-1 inhibitor

    ABT-046 is a potent, selective, and orally bioavailable Diacylglycerol acyltransferase 1 (DGAT-1 ) inhibitor (IC50= 8 nM).
  44. Hsp90 inhibitor

    Alvespimycin is a selective Hsp90 inhibitor with a GI50 of 53 nM.
  45. FLAP inhibitor

    AM679 is a potent and selective FLAP inhibitor with IC50s of 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively.
  46. CYP3A4 Inhibitor

    Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA.
  47. DGAT1 inhibitor

    AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1).
  48. CYP2C19/CYP2B6 inhibitor

    Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia.
  49. DGAT-1 inhibitor

    DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.
  50. Factor Xa inhibitor

    Edoxaban is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.

Items 251-300 of 756

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