Metabolism

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Product Information
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  1. ATX inhibitor

    ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, FS-3 and 2.18 nM, bis-pNPP) inhibitor.
  2. SCD inhibitor

    T-3764518 is a novel and potent stearoyl coenzyme A desaturase (SCD) inhibitor with an IC50 of 4.7 nM.
  3. PCSK9 inhibitor

    SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1, Figure 1.
  4. PDE5 inhibitor

    ER21355 is an inhibitor of phosphodiesterase 5 (PDE5), used for treatment of prostatic diseases.
  5. ACE inhibitor

    Rentiapril is an orally active angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity.
  6. FAAH inhibitor

    FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor, with IC50s of 145 nM and 650 nM for rat and human FAAH, respectively.
  7. LOXL2 inhibitor

    PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor.
  8. pan HDAC inhibitor

    Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
  9. aspartyl-tRNA synthetase inhibitor

    Asp-AMS, an analogue of aspartyl-adenylate, is an aspartyl-tRNA synthetase inhibitor and also a strong competitive inhibitor of the mitochondrial enzyme.
  10. ACDase inhibitor

    LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
  11. FASN inhibitor

    HS-79 is an enantiomer of Fasnall, which is a selective fatty acid synthase (FASN) inhibitor. HS-79 is able to inhibit the incorporation of tritiated acetate into lipids with an IC50 of 1.57 μM.
  12. PDE3 inhibitor

    LAS-31180 is an inhibitor of phosphodiesterase 3, with positive inotropic and vasodilator properties.
  13. DGAT1 inhibitor

    Diacylglycerol acyltransferase inhibitor-1 is a diacylglycerol acyltransferase (DGAT1) inhibitor.
  14. LDHA inhibitor

    GSK2837808A is a potent and selective lactate dehydrogenase A (LDHA) inhibitor with IC50s of 1.9 and 14 nM for LDHA and LDHB, respectively.
  15. GCase inhibitor

    Conduritol B epoxide is an irreversible covalently bound acid β-glucosidase (GCase) inhibitor.
  16. PDE1 inhibitor

    PDE1-IN-2 is an inhibitor of PDE1 extracted from patent WO2016/55618 A1, example 31; has IC50 values of 6, 140 and 164 nM for PDE1C, PDE1B and PDE1A, respectvely.
  17. PDE5 inhibitor

    MY-5445 is a specific phosphodiesterase type 5 (PDE5) inhibitor.
  18. PDE-4 inhibitor

    Roflumilast Impurity E is the impurity of Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.
  19. sEH inhibitor

    TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.
  20. CYP1B1 inhibitor

    DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
  21. CYP1B1 inhibitor

    DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
  22. PDE inhibitor

    Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM.
  23. NAMPT inhibitor

    LB-60-OF61 is a NAMPT inhibitor and is a cytotoxic compound with a selectivity towards MYC overexpressing cell lines.
  24. GCN2 inhibitor

    GCN2-IN-1 (A-92) is a potent general control nonderepressible 2 kinase (GCN2) inhibitor with an IC50 of <0.3 μM in the enzyme assay and an IC50 of 0.3-3 μM in the cell assay.
  25. ABHD6 inhibitor

    JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
  26. STK16 kinase inhibitor

    STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.
  27. fumarate hydratase inhibitor

    Fumarate hydratase-IN-1 (compound 2) is a cell-permeable fumarate hydratase inhibitor. Fumarate hydratase-IN-1 has antiproliferative activity against several cancer cell lines with a mean IC50 of 2.2 μM.
  28. SCD1 inhibitor

    XEN723 is a novel and potent thiazolylimidazolidinone inhibitor of Stearoyl-CoA Desaturase (SCD1) with IC50s of 45 and 524 nM in mouse and HepG2 cell, respectively.
  29. NO synthase inhibitor

    Agmatine sulfate exerts modulatory action at multiple molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor.
  30. PDE4 inhibitor

    CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively.
  31. aldosterone synthase inhibitor

    BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
  32. mPTP opening inhibitor

    ER-000444793 is a potent inhibitor of mitochondrial permeability transition pore (mPTP) opening. ER-000444793 inhibits mPTP with an IC50 of 2.8?μM.
  33. fXIa inhibitor

    FXIa-IN-1 (compound EP-7041) is a potent β-lactam covalent heparin-derived factor XIa (fXIa) inhibitor.
  34. dual PDE7/GSK-3 inhibitor

    VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
  35. IDO/TDO dual inhibitor

    IDO/TDO-IN-1 is a highly potent and orally active dual indoleamine-2,3-dioxygenase (IDO) and tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50s of 9.7 and 47 nM, respectively .
  36. EMT inhibitor

    EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
  37. Hsp47 inhibitor

    Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix.
  38. FT/GGT dual inhibitor

    FGTI-2734 is a RAS C-terminal mimetic dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitor with IC50s of 250 nM and 520 nM for FT and GGT, respectively.
  39. PDE12 inhibitor

    PDE12-IN-3 is a phosphodiesterase 12 (PDE12) inhibitor with a pXC50 of 7.68. Antiviral activity.
  40. PDE 10A inhibitor

    MT-3014 is a potent, highly selective and brain-penetrated phosphodiesterase 10A (PDE 10A) inhibitor, with IC50s of 0.062 nM and 0.09 nM for human PDE 10A and bovine PDE 10A, respectively.
  41. cNIIIB nucleotidase inhibitor

    7-Methylguanosine is a novel cNIIIB nucleotidase inhibitor with IC50 value of 87.8????7.5??M.
  42. 5-Lipoxygenase (5-LO) inhibitor

    Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation.
  43. Serine/arginin kinase 1 inhibitor

    SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50 = 5.9 nM).
  44. MAGL inhibitor

    ABX-1431 is a highly potent, selective, and orally available, CNS-penetrant monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 14 nM.
  45. AAK1 inhibitor

    LP-935509 is a potent inhibitor of the Adapter protein-2 Associated Kinase 1 (AAK1).
  46. PDE4D inhibitor

    BPN14770 is a selective phosphodiesterase 4D (PDE4D) allosteric inhibitor with IC50s of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively.
  47. uPA inhibitor

    ZK824859 is an oral available and selective urokinase plasminogen activator (uPA) inhibitor with IC50s of 79?nM, 1580?nM and 1330?nM for human uPA, tPA, and plasmin, respectively.
  48. FXIa inhibitor

    BMS-962212 is a reversible, direct, and highly selective inhibitor of FXIa.
  49. PDE5/HDAC-1 inhibitor

    CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer??s disease.
  50. cell motility and cell invasion inhibitor

    KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.

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