Metabolism

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  1. SGK inhibitor

    EMD638683 is a potent inhibitor of SGK1 with an IC50 value of 3 uM.
  2. PDE Inhibitor

    GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.
  3. FLAP inhibitor

    MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay.
  4. FLAP inhibitor

    MK591 is selective and specific inhibitor of 5-Lipoxygenase-activating protein (FLAP).
  5. Liver-targeting SCD Inhibitor

    MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy.
  6. lipoxygenase inhibitor

    Nordihydroguaiaretic acid is a natural phenolic compound isolated from the creosote bush Larrea divaricata, which has anti-tumor activities both in vitro and in vivo. Its analogs are in clinical development for use in refractory solid tumors.
  7. PDE5 inhibitor

    Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
  8. PDE4 inhibitor

    Oglemilast is a potent inhibitor of PDE4.
  9. PDE3 inhibitor

    Olprinone is a selective phosphodiesterase 3 (PDE3) inhibitor.
  10. DHFR inhibitor

    Pemetrexed is a novel antifolate and antimetabolite for TS, DHFR and GARFT with Ki of 1.3 nM, 7.2 nM and 65 nM, respectively.
  11. FAAH inhibitor

    PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.
  12. Hsp90 inhibitor

    Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.
  13. Cathepsin K Inhibitor

    L006235 is a potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S.
  14. Human cathepsin L inhibitor

    SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G.
  15. FASN Inhibitor

    C 75 is an inhibitor of fatty acid synthase (FAS) reducing food intake and body weight in mice.
  16. Suppressor of mitochondrial apoptosis

    iMAC2 inhibits mitochondrial apoptosis-induced channel (MAC) (IC50 = 28 nM).
  17. elastogenesis inhibitor

    L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor.
  18. PAK4/NAMPT Inhibitor

    KPT 9274 ( ATG-019) is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay.
  19. Autotaxin Inhibitor

    HA130 is a selective autotaxin (ATX) inhibitor with an IC50 of 28 nM.
  20. GLUT1 Inhibitor

    STF-31 is an inhibitor of glucose transporter 1 (GLUT1, IC50 = 1 muM),
  21. IDO inhibitor

    Epacadostat is a potent and selective indoleamine 2,3-dioxygenase (IDO1) inhibitor with IC50 of 10 nM, Phase 2,
  22. LXRα inhibitor

    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
  23. HDAC/ACE inhibitor

    Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity. Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells.
  24. Cathepsin S inhibitor

    LY3000328 is a Cathepsin S inhibitor with excellent in vitro potency and selectivity against other cysteine proteases.
  25. MAO inhibitor

    Olodaterol is a long acting beta-adrenoceptor agonist used as an inhalation for treating patients with chronic obstructive pulmonary disease (COPD), manufactured by Boehringer-Ingelheim.
  26. FPTase inhibitor

    L-778123 HCl is an inhibitor of FPTase and GGPTase-I with IC50 of 2 nM and 98 nM in enzyme inhibition determination.
  27. 15-PGDH enzyme inhibitor

    SW033291 is a small-molecule inhibitor of 15-PGDH (Ki=0.1 nM) that increases prostaglandin PGE2 levels in bone marrow and other tissues.
  28. PDE10A inhibitor?€?

    TAK-063 is a highly potent, selective and orally active PDE10A inhibitor with IC50 of 0.30 nM; >15000-fold selectivity over other PDEs.
  29. IDH2 inhibitor

    Enasidenib is a potent and selective IDH2 inhibitor with potential anticancer activity (IDH2 = Isocitrate dehydrogenase 2).
  30. ACL inhibitor and AMPK activator

    ETC-1002 is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
  31. FLAP inhibitor

    GSK2190915 is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding IC50 of 2.9 nM.
  32. cytochrome P450 inhibitor

    Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI).
  33. Carbonic Anhydrase Inhibitor

    Acetazolamide, a potent carbonic anhydrase (CA) inhibitor, is commonly used in clinical practice as an immediate and readily available option for acute reduction of intraocular pressure(IOP).
  34. Ferroptosis inhibitor

    RSL3 is a ferroptosis activator in a VDAC-independent manner,exhibiting selectivity for tumor cells bearing oncogenic RAS.
  35. Dehydrogenase Inhibitor

    AG-120 is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity.
  36. Foxo1 Inhibitor

    AS1842856 is a cell-permeable inhibitor that blocks the transcription activity of Foxo1 with IC50 of 33 nM. It could directly bind to the active Foxo1, but not the Ser256-phosphorylated form.
  37. Glucose Transporter Inhibitor I

    WZB117 is an inhibitor of Glucose Transporter 1 (GLUT1). It inhibited cell proliferation in lung cancer A549 cells and breast cancer MCF7 cells with an IC50 of approximately 10 uM.
  38. hALDH1 Inhibitor

    NCT-501 is a potent and selective inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1) with IC50 of 40 nM.
  39. COX inhibitor

    Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects.
  40. STK33 inhibitor

    ML-281 is a potent ans selective STK33 inhibitor with IC50 value of 14 nM.
  41. 3PO

    PFKFB3 inhibitor

    3PO is a PFKFB3 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase) inhibitor.
  42. lipase inhibitor

    Cetilistat is a drug designed to treat obesity. It acts in the same way as the older drug orlistat (Xenical) by inhibiting pancreatic lipase, an enzyme that breaks down triglycerides in the intestine.
  43. FAAH inhibitor

    JNJ-42165279 is a potent and selective fatty acid amide hydrolase (FAAH) inhibitor.
  44. TPPII inhibitor

    Butabindide oxalate is a selective and potent inhibitor of TPPII (tripeptidyl peptidase II).
  45. HSP90 inhibitor

    Gedunin, a naturally occurring Hsp90 inhibitor, is tetranortriterpenoid isolated from the Indian neem tree (Azadirachta indica).
  46. HSP90 inhibitor

    Macbecin I is an ansamycin antibiotic compound that inhibits Hsp90 activity with IC50 value of μM by binding to the ATP-binding site.
  47. HSP90 inhibitor

    EC 144 is a potent inhibitor of the heat shock protein 90 and was found to be effective in tumor growth suppression.
  48. SINE inhibitor

    KPT 335 is an orally bioavailable Selective Inhibitor of Nuclear Export (SINE).
  49. MAGL inhibitor

    MJN110 is a potent selective inhibitor of MAGL, the enzyme predominantly responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) with >10,000 selectivity over FAAH, the hydrolase that degrades the endocannabinoid anandamide (AEA).
  50. SREBP inhibitor

    Fatostatin Hydrobromide is an inhibitor of sterol regulatory element-binding protein (SREBP).

Items 301-350 of 756

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