Metabolism

Items 401-450 of 5815

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  1. cytochrome P450 substrate

    Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.
  2. Nicotinuric acid is an acyl glycine. Nicotinuric acid is a metabolite of nicotinic acid.
  3. YZ9

    PFKFB3 inhibitor

    YZ9 is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor with IC50 value of 0.183 μM.
  4. cathepsin S inhibitor

    Petesicatib is a cathepsin S inhibitor, used in research of immune diseases.
  5. Isotetrandrine is a biscoclaurine alkaloid inhibitor of G protein activation of PLA2 but not PLC or PLD.
  6. Xanthine oxidase inhibitor

    Oxipurinol (Oxipurinol), the major active metabolite of Allopurinol, is an inhibitor of xanthine oxidase. Oxipurinol can be used to regulate blood urate levels and treat gout.
  7. Lathosterol is a cholesterol-like molecule. Serum Lathosterol concentration is an indicator of whole-body cholesterol synthesis.
  8. 7-Methylguanine is a metabolite of DNA methylation. It can be generated by methylating agents, and used as a probe of protein?CDNA interactions and a key component of DNA sequencing method.
  9. PDE4 inhibitor

    MK-0359 is a selective and potent oral PDE4 inhibitor, in chronic asthma.
  10. Cathepsin S inhibitor

    Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.

     
  11. hIDO2 inhibitor

    GNF-PF-3777 (8-Nitrotryptanthrin) is a potent human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
  12. CYP17A1/androgen synthesis inhibitor

    Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues.
  13. Glucokinase activator

    Piragliatin is a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus
  14. α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
  15. HSD1 inhibitor

    AZD4017 is a potent, selective, and orally bioavailable11b-HSD1 inhibitor (11b-hydroxysteroid dehydrogenase type 1 inhibitor).
  16. Cathepsin B inhibitor

    CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.
  17. Carbonic anhydrase inhibitor

    Benzenesulfonamide ia an inhibitor of carbonic anhydrases.
  18. PDE3 inhibitor

    Cilostamide is a selective inhibitor of phosphodiesterase (PDE)3A and PDE3B with IC50 values of 27 and 50 nM, respectively.
  19. PDE9A Inhibitor

    PDE9-IN-1 is a potent, selective, and orally bioavailable phosphodiesterase-9A (PDE9A) Inhibitor with an IC50 of 8.7 nM.
  20. HSP90-calcineurin-NFAT inhibitor

    YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation.
  21. 8-Hydroxyguanine is a major pre-mutagenic lesion generated from reactive oxygen species. It causes G-T and A-C substitutions.
  22. cathepsin C substrate

    Gly-Phe-beta-naphthylamide is a cathepsin C substrate. The compound is described to accumulate inside lysosomes leading to their destruction.
  23. ACE inhibitor

    Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM.
  24. FP-Biotin is a biotinylated organophosphorus agent. It could be useful for identifying proteins that react with organophosphorus toxicants (OP).
  25. Geranylgeranylacetone can induce expression of HSP70, HSPB8, and HSPB1.
  26. Atovaquone is an anti-protozoal mitochondrial electron transport inhibitor.
  27. HMG-CoA reductase inhibitor

    Mevastatin is an inhibitor of HMG-CoA reductase.
  28. CCK antagonist

    Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini.
  29. PDE-KRAS inhibitor

    Deltarasin is a novel small molecule inhibiting the KRAS PDEδ interaction and thus impairing oncogenic KRAS signalling.
  30. PGC-1α regulator

    ZLN005 is a PGC-1α Transcriptional Regulator, which shoed some beneficialfEffects on diabetic db/db mice.
  31. Turanose is a reducing disaccharide.
  32. HMG-CoA reductase inhibitor

    Atorvastatin is an HMG-CoA reductase inhibitor (IC50 = 154 nM) that is effective in treating hypercholesterolemia and certain dyslipidemias.
  33. MAGL inhibitor

    JW-642 is a potent inhibitor of monoacylglycerol lipase (MAGL) that displays IC50 values of 7.6, 14, and 3.7 nM for inhibition of MAGL in mouse, rat, and human brain membranes, respectively.
  34. Glucokinase activator

    Glucokinase activator 1 is a liver-directed glucokinase activator with an EC50 of 34 nM.
  35. Vatiquinone is a new drug that is based on vitamin E.
  36. ATP-citrate lyase inhibitor

    BMS303141 is a potent inhibitor of ATP citrate lyase (ACL). BMS303141 inhibits lipid synthesis in HepG2 cells with an IC50 of 8 μM, and lowers plasma triglycerides in a murine hyperlipdemia model.
  37. Hsp90 inhibitor

    VER-49009 is a pyrazole compound that inhibits Hsp90 with an IC50 value of 47 nM.
  38. 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.
  39. Hsp90 inhibitor

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

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
  41. 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).
  42. FXR agonist

    Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM
  43. NS5B Inhibitor

    ABT333 is an NS5B non-nucleoside polymerase inhibitor.
  44. 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).
  45. HMG-CoA reductase inhibitor

    Pitavastatin Lactone is an HMG-CoA reductase inhibitor.
  46. 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.
  47. 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.
  48. 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.
  49. FTase inhibitor

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

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

Items 401-450 of 5815

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