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Metabolism

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Items 51-100 of 2992

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  1. A18015
    Edoxaban

    factor Xa (FXa) inhibitor

    Edoxaban(DU-176) is an oral factor Xa (FXa) inhibitor in clinical development for stroke prevention.
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  2. A10011
    17-DMAG HCl (Alvespimycin)

    Hsp90 inhibitor

    17-DMAG is a water-soluble analog of 17-AAG and geldanamycin that binds the ATP binding site of Hsp90 and inhibits its chaperone activity. Displays more potent antitumor activity than 17-AAG.
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  3. A13822
    Erastin

    VDAC inhibitor

    Erastin is a cell-permeable piperazinyl-quinazolinone compound that exhibits oncogene-selective lethality in cells with H-Ras mutations.
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  4. A13593
    CA-074 Methyl Ester

    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.
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  5. A12850
    HSP-990

    HSP90 Inhibitor

    HSP990 is an orally bioavailable inhibitor of human heat-shock protein 90 (Hsp90) with potential antineoplastic activity.
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  6. A11189
    SNX-2112

    Hsp90 inhibitor

    SNX-2112 is a heat shock protein 90 (Hsp90) inhibitor with anticancer properties currently in clinical trials. SNX-2112 induced autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and autophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent

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  7. A11130
    Zelavespib (PU-H71)

    Hsp90 Inhibitor

    PU-H71 is a potent Hsp90 inhibitor (IC50 = 50 nM).
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  8. A11403
    MK-8245

    SCD inhibitor

    MK-8245 is a Liver-Targeted Stearoyl-CoA Desaturase (SCD) Inhibitor. MK-8245 is useful for the Treatment of Diabetes and Dyslipidemia.
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  9. A18734
    JG-98

    Hsp70 inhibitor

    JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
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  10. A15808
    Enasidenib

    IDH2 inhibitor

    Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).
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  11. A11131
    MPC-3100

    Hsp90 inhibitor

    MPC-3100 is an orally bioavailable, synthetic, second-generation small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
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  12. A10143
    BIIB021

    HSP90 inhibitor

    BIIB021 is an oral fully synthetic Hsp90 inhibitor that selectively and potently inhibits the molecular chaperone Hsp90 thereby inhibiting the proper assembly of multiple oncogenic proteins involved in tumor growth and survival.
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  13. A20475
    ML-210

    GPX4 inhibitor

    ML-210??the most potent compound in the nitroisoxazole series?? is a selective covalent inhibitor of glutathione peroxidase 4 (GPX4) by binding the selenocysteine residue.
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  14. A11786
    CPI-613 (Devimistat)

    Dehydrogenase Inhibitor

    CPI-613 is a racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities.
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  15. A15919
    Xanthohumol

    COX inhibitor

    Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.
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  16. A17216
    BAY-876

    GLUT1 Inhibitor

    BAY-876 is a potent and Selective GLUT1 Inhibitor. BAY-876 showed good metabolic stability in vitro and high oral bioavailability in vivo.
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  17. A14190
    Tiplaxtinin (PAI-039)

    PAI-1 inhbitor

    Tiplaxtinin is a selective and orally efficacious inhibitor of plasminogen activator inhibitor-1 (PAI-1) with IC50 of 2.7 μM.
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  18. A10805
    Rolipram

    PDE4 inhibitor

    Rolipram is a PDE4-inhibitor with IC50 = 2.0 μM.
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  19. A11199
    A 922500

    DGAT-1 inhibitor

    A 922500 is a diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively).

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  20. A11697
    Licofelone

    COX/LOX inhibitor

    Licofelone is a dual COX/LOX inhibitor, being considered as a treatment for osteoarthritis. It may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase). Licofelone is the first drug to inhibit both.
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  21. A10800
    Rivaroxaban (Xarelto)

    Factor Xa inhibitor

    Rivaroxaban is an oxazolidinone derivative optimized for inhibiting both free Factor Xa and Factor Xa bound in the prothrombinase complex.
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  22. A12328
    Lonafarnib (SCH66336)

    FPTase inhibitor

    Lonafarnib (SCH 66336) is a selectively FPTase inhibitor for H-ras, K-ras-4B and N-ras with IC50 of 1.9 nM, 5.2 nM and 2.8 nM, respectively.
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  23. 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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  24. A11025
    Geldanamycin

    Hsp90 inhibitor

    Geldanamycin binds to the ATP site of Hsp90 (Kd = 1.2 μM) and inhibits its chaperone activity.
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  25. A10669
    Oligomycin A

    ATPase inhibitor

    Oligomycin A is a mitochondrial ATPase inhibitor. Oligomycin A inhibits ATP5 (mitochondrial ATPases, F1F0) bound to the cell membrane.
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  26. A13256
    CA-074

    Cathepsin B inhibitor

    CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.
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  27. A12833
    Ro 61-8048

    Hydroxylase Inhibitor

    Ro 61-8048 is a potent and competitive kynurenine 3-hydroxylase inhibitor (Ki = 4.8 nM, IC50 = 37 nM).
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  28. A10054
    Alizarin

    CYP17 inhibitor

    Alizarin is novelly used as a staining agent in biological research because it stains free calcium and certain calcium compounds a red or light purple color.
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  29. A11517
    Otamixaban (FXV 673)

    factor Xa inhibitor

    Otamixaban(FXV 673) is an intravenous direct factor Xa inhibitor.
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  30. A11289
    Apremilast (CC 10004)

    PDE4 Inhibitor

    Apremilast, a novel PDE4 inhibitor, inhibits spontaneous production of tumour necrosis factor-alpha from human rheumatoid synovial cells and ameliorates experimental arthritis.
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  31. A13363
    Metyrapone

    Cytochrome P450 inhibitor

    Metyrapone is an inhibitor of cytochrome P450-mediated ω/ω-1 hydroxylase activity and CYP11B1.
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  32. A15331
    C-75 Trans

    FASN Inhibitor

    C 75 is an inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice.
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  33. A17555
    Ciprofloxacin hydrochloride hydrate

    Topoisomerase IV inhibitor

    Ciprofloxacin Hydrochloride is a broad-spectrum antimicrobial carboxyfluoroquinoline, interfering with the bacterial DNA gyrase, inhibiting the DNA synthesis, and preventing bacterial cell growth.
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  34. A10120
    Baicalein

    Lipoxygenase Inhibitor

    Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.

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  35. 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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  36. A10935
    Tipifarnib (Zarnestra)

    FTase inhibitor

    Tipifarnib (Zarnestra) is a farnesyltransferase inhibitor that inhibits the Ras kinase in a post translational modification step before the kinase pathway becomes hyperactive.
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  37. A15932
    3PO

    PFKFB3 inhibitor

    3PO is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor.
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  38. A10548
    LY315920 (Varespladib)

    HnsPLA inhibitor

    LY315920 (Varespladib) is an inhibitor of the IIa, V, and X isoforms of secretory phospholipase A2 (sPLA2).
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  39. A20462
    TM5275 sodium

    plasminogen activator inhibitor

    TM5275 sodium is a plasminogen activator inhibitor (PAI-1) with an IC50 of 6.95 μM.
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  40. A22275
    Sodium oxamate

    LDH inhibitor

    Sodium oxamate (SO, Aminooxoacetic acid, Oxamic acid) is an inhibitor of lactate dehydrogenase (LDH) that specificly inhibits LDH?A.
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  41. A12582
    Selinexor (KPT-330)

    CRM1 inhibitor

    KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia.
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  42. A12631
    Sildenafil

    PDE5 inhibitor

    Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors(IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.
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  43. A10010
    Tanespimycin (17-AAG, KOS953)

    HSP90 inhibitor

    17-AAG is an ansamycin antibiotic which acts as an anti-tumor agent. Specifically, 17-AAG binds and inhibits Hsp90.
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  44. A10102
    Avasimibe (CI-1011)

    CYP17 inhibitor

    Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor.
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  45. A12125
    (Rac)-Shikonin

    PTEN Inhibitor

    Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.
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  46. A12648
    CUDC-305 (DEBIO-0932 )

    HSP90 inhibitor

    Debio 0932 is a novel heat shock protein 90 (HSP90) inhibitor with strong affinity for HSP90 alpha/beta, high oral bioavailability and potent anti-proliferative activity against a broad range of cancer cell lines (with a mean IC50 of 220 nmol/L), including many non-small cell lung cancer (NSCLC) cell lines which are resistant to standard-of-care (SOC) agents.
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  47. A11251
    XL-888

    HSP90 Inhibitor

    XL888 is an orally bioavailable, ATP-competitive, small-molecule inhibitor of heat shock protein 90 (Hsp90) with potential antineoplastic activity.
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  48. A12301
    ML349

    APT-2 inhibitor

    ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
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  49. A12303
    Bergaptol

    CYP3A4 enzyme inhibitor

    Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties.
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  50. A12318
    SC-26196

    δ6 desaturase inhibitor

    Selective δ6 desaturase inhibitor (IC50 = 0.2 μM in vitro).
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