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P450

Cytochrome P450 are a family of heme-containing monoxygenases catalyzing the metabolism of xenobiotics in the body where P450 enzymes use O2 and two electrons provided by NAD(P)H with the help of redox partner flavoproteins and iron-sulfur proteins to catalyze the monooxygenation of a variety of substrates. Based on how electrons from NAD(P)H are delivered to the catalytic site, P450 enzymes are divided into four classes, including Class I requiring both an FAD-containing reductase and an iron sulfur redoxin, Class II requiring only an FAD/FMN-containg P450 reductase, Class III requiring no electron donor and Class IV requiring electrons directly from NAD(P)H.

Products for  P450

  1. Cat.No. Product Name Information
  2. GC66197 α-?Terpinyl acetate α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM. α-?Terpinyl acetate  Chemical Structure
  3. GC45239 δ4-Abiraterone δ4-Abiraterone is a major metabolite of abiraterone. δ4-Abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor. δ4-Abiraterone  Chemical Structure
  4. GC49875 (±)-N-desmethyl Venlafaxine (hydrochloride) A minor active metabolite of venlafaxine (±)-N-desmethyl Venlafaxine (hydrochloride)  Chemical Structure
  5. GC12404 (+)-Ketoconazole Potent inhibitor of cytochrome P450c17 (+)-Ketoconazole  Chemical Structure
  6. GC30424 (-)-Cephaeline dihydrochloride (NSC 32944) (-)-Cephaeline dihydrochloride (NSC 32944) is a selective CYP2D6 inhibtor with an IC50 of 121 μM. (-)-Cephaeline dihydrochloride (NSC 32944)  Chemical Structure
  7. GC14486 (S)-Mephenytoin

    S-Mephenytoin is an anticonvulsive drug which is metabolized by N-demethylation and 4-hydroxylation .

    (S)-Mephenytoin  Chemical Structure
  8. GC33073 1-Ethynylnaphthalene 1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. 1-Ethynylnaphthalene  Chemical Structure
  9. GC13836 2,3-dihydrothieno-Thiadiazole Carboxylate CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor 2,3-dihydrothieno-Thiadiazole Carboxylate  Chemical Structure
  10. GC12262 2-Phenyl-2-(1-piperidinyl)propane mechanism-based inactivator of human cytochrome P450 (CYP) 2B6 2-Phenyl-2-(1-piperidinyl)propane  Chemical Structure
  11. GC33071 4'-Methylchrysoeriol 4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD. 4'-Methylchrysoeriol  Chemical Structure
  12. GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes. 4-(Trifluoromethyl)umbelliferone  Chemical Structure
  13. GC11758 4-phenyl-5-methyl-1,2,3-Thiadiazole CYP2B4 and CYP2E1 inhibitor 4-phenyl-5-methyl-1,2,3-Thiadiazole  Chemical Structure
  14. GN10241 5-Methoxypsoralen 5-Methoxypsoralen  Chemical Structure
  15. GC35201 8-Geranyloxypsoralen 8-Geranyloxypsoralen is a furanocoumarin isolated from grapefruit, acts as a potent inhibitor of P450 3A4 (CYP3A4) with an IC50 of 3.93 μM. 8-Geranyloxypsoralen  Chemical Structure
  16. GN10330 8-Methoxypsoralen 8-Methoxypsoralen  Chemical Structure
  17. GC17645 Abiraterone A CYP17A1 inhibitor and an active metabolite of abiraterone acetate Abiraterone  Chemical Structure
  18. GC11108 Abiraterone acetate A CYP17A1 inhibitor Abiraterone acetate  Chemical Structure
  19. GC64010 Abiraterone decanoate Abiraterone decanoate is a potent Abiraterone prodrug. Abiraterone decanoate provide a controlled release of Abiraterone and long-acting CYP17 inhibition with intramuscular (IM) delivery. Abiraterone decanoate  Chemical Structure
  20. GC14781 ABT (1-Aminobenzotriazole) ABT (1-Aminobenzotriazole) is a nonspecific and irreversible inhibitor of cytochrome P450 (P450). ABT (1-Aminobenzotriazole)  Chemical Structure
  21. GC35236 Acetylshikonin Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin  Chemical Structure
  22. GC16575 Alizarin A CYP450 inhibitor Alizarin  Chemical Structure
  23. GC31141 Antihistamine-1 Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively. Antihistamine-1  Chemical Structure
  24. GN10150 Apigenin Apigenin (API) is a competitive CYP2C9 inhibitor with a Ki of 2 µM.. Apigenin  Chemical Structure
  25. GC12945 Atazanavir An inhibitor of HIV-1 protease Atazanavir  Chemical Structure
  26. GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease Atazanavir sulfate (BMS-232632-05)  Chemical Structure
  27. GC65088 Atovaquone-d5 Atovaquone-d5  Chemical Structure
  28. GC10999 Avasimibe An ACAT inhibitor Avasimibe  Chemical Structure
  29. GC34132 Bergamottin (5-Geranoxypsoralen) Bergamottin (5-Geranoxypsoralen) is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM. Bergamottin (5-Geranoxypsoralen)  Chemical Structure
  30. GC33909 Bergaptol (5-Hydroxypsoralen) Bergaptol (5-Hydroxypsoralen) is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Bergaptol (5-Hydroxypsoralen)  Chemical Structure
  31. GC65345 BI 653048 BI 653048 is a selective and orally active nonsteroidal?glucocorticoid (GC)?agonist with an IC50 value of 55 nM. BI 653048  Chemical Structure
  32. GC32419 BI 689648 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. BI 689648  Chemical Structure
  33. GC31479 BMS-819881 BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM. BMS-819881  Chemical Structure
  34. GC32257 Carbosulfan Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan  Chemical Structure
  35. GC31464 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. CDD3505  Chemical Structure
  36. GC31460 CDD3506 CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. CDD3506  Chemical Structure
  37. GC32991 Cecropin B Cecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic. Cecropin B  Chemical Structure
  38. GC38681 Cedrol A sesquiterpene alcohol Cedrol  Chemical Structure
  39. GC16751 Chlorzoxazone Muscle-relaxing drug Chlorzoxazone  Chemical Structure
  40. GC11170 Choline Fenofibrate Choline Fenofibrate  Chemical Structure
  41. GC35692 Chrysosplenetin A flavonoid with diverse biological activities Chrysosplenetin  Chemical Structure
  42. GC16754 Clarithromycin A macrolide antibiotic Clarithromycin  Chemical Structure
  43. GC38758 Clomethiazole Chlormethiazole is an potent and orally active GABAA?agonist. Clomethiazole  Chemical Structure
  44. GC14269 Cobicistat (GS-9350) An inhibitor of CYP3A Cobicistat (GS-9350)  Chemical Structure
  45. GN10338 Compound K Compound K  Chemical Structure
  46. GC41611 Curcumenol Curcumenol is a sesquiterpene that has been found in Curcuma species. Curcumenol  Chemical Structure
  47. GC35788 CYP17-IN-1 CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM. CYP17-IN-1  Chemical Structure
  48. GC35803 Dafadine-A Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1). Dafadine-A  Chemical Structure
  49. GC63872 Dagrocorat hydrochloride Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride  Chemical Structure
  50. GC49817 Desethoxy Quetiapine (hydrochloride) An active metabolite of quetiapine Desethoxy Quetiapine (hydrochloride)  Chemical Structure
  51. GC49866 Desmethyl Carvedilol An active metabolite of carvedilol Desmethyl Carvedilol  Chemical Structure
  52. GC49842 Digoxigenin Bisdigitoxoside A Na+/K+-ATPase inhibitor Digoxigenin Bisdigitoxoside  Chemical Structure
  53. GC30479 Dihydromethysticin ((+)-Dihydromethysticin) Dihydromethysticin ((+)-Dihydromethysticin) is one of the six major kavalactones found in the kava plant; has marked activity on the induction of CYP3A23. Dihydromethysticin ((+)-Dihydromethysticin)  Chemical Structure
  54. GC16550 Diosmetin CYP1A1 inhibitor Diosmetin  Chemical Structure
  55. GC19415 DMU2105 DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively. DMU2105  Chemical Structure
  56. GC19416 DMU2139 DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively. DMU2139  Chemical Structure
  57. GC12892 Doxepin (hydrochloride) histamine, serotonin, adrenergic, and muscarinic receptors antagonist Doxepin (hydrochloride)  Chemical Structure
  58. GC65260 EDP-305 EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305  Chemical Structure
  59. GC35981 EMT inhibitor-2 EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2  Chemical Structure
  60. GC12250 Fenofibrate

    PPARα agonist

    Fenofibrate  Chemical Structure
  61. GC38623 Fraxinol Fraxinol is isolated from Lobelia chinensis. Fraxinol  Chemical Structure
  62. GC32855 Furafylline

    Furafylline, as a long-acting replacement for theophylline in the treatment of asthma, is a methylxanthine derivative[1].

    Furafylline  Chemical Structure
  63. GN10137 Galangin Galangin  Chemical Structure
  64. GC14915 Gemfibrozil PPARα activator Gemfibrozil  Chemical Structure
  65. GN10720 Gentiopicrin Gentiopicrin  Chemical Structure
  66. GN10032 Ginsenoside F1 Ginsenoside F1  Chemical Structure
  67. GN10549 Ginsenoside Rd Ginsenoside Rd  Chemical Structure
  68. GC39168 GSK2945 hydrochloride GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride  Chemical Structure
  69. GC49855 Harmalol (hydrochloride hydrate) A β-carboline alkaloid and an active metabolite of harmaline Harmalol (hydrochloride hydrate)  Chemical Structure
  70. GC11540 HET0016 inhibitor of 20-HETE formation HET0016  Chemical Structure
  71. GC49832 Hydroxymetronidazole Hydroxymetronidazole (Metronidazole-OH) is a metabolite of Metronidazole belonging to the class of nitroimidazoles. Hydroxymetronidazole  Chemical Structure
  72. GC16707 Isavuconazole triazole antifungal drug Isavuconazole  Chemical Structure
  73. GC36335 Isoglycycoumarin Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin  Chemical Structure
  74. GN10568 Isosilybin Isosilybin  Chemical Structure
  75. GC17337 Ketoconazole A triazole antifungal agent Ketoconazole  Chemical Structure
  76. GC38554 Liarozole dihydrochloride

    ?Liarozole dihydrochloride is a P-450 inhibitor and retinoic acid (RA) metabolizing blocking agent inhibits RA metabolism and thereby increases intracellular RA levels in cells that actively produce RA.

    Liarozole dihydrochloride  Chemical Structure
  77. GC67933 LKY-047 LKY-047  Chemical Structure
  78. GC31422 MCH-1 antagonist 1

    MCH-1 antagonist 1 is a potent melanin concentrating hormone (MCH-1) antagonist with a Ki of 2.6 nM.

    MCH-1 antagonist 1  Chemical Structure
  79. GC10198 Memantine hydrochloride NMDA receptor antagonist Memantine hydrochloride  Chemical Structure
  80. GC41373 Methysticin Methysticin is a kavalactone isolated from the kava roots. Methysticin  Chemical Structure
  81. GC17411 Metyrapone 11-β hydroxylase (CYP11B1) inhibitor Metyrapone  Chemical Structure
  82. GC16423 Monoacetylphloroglucinol Monoacetylphloroglucinol (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity. Monoacetylphloroglucinol  Chemical Structure
  83. GC36754 N-Nornuciferine N-Nornuciferine is an aporphine alkaloid in lotus leaf that significantly inhibits CYP2D6 with IC50 and Ki of 3.76 and 2.34 μM, respectively. N-Nornuciferine  Chemical Structure
  84. GN10257 Naringin Naringin  Chemical Structure
  85. GC49851 Norquetiapine An active metabolite of quetiapine Norquetiapine  Chemical Structure
  86. GC69602 Obtusifoliol

    Obtusifoliol is a specific CYP51 inhibitor, with Kd values of 1.2 μM and 1.4 μM for the affinity to Brucella melitensis (TB) and human CYP51, respectively.

    Obtusifoliol  Chemical Structure
  87. GC30966 Olivetol Olivetol is a naturally phenol found in lichens and produced by certain insects, acting as a competitive inhibitor of the cannabinoid receptors CB1 and CB2. Olivetol  Chemical Structure
  88. GC11155 Omeprazole sulfone Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor. Omeprazole sulfone  Chemical Structure
  89. GC36822 Oteseconazole Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51. Oteseconazole  Chemical Structure
  90. GC12280 PF-4981517 A potent, selective inhibitor of CYP3A4 PF-4981517  Chemical Structure
  91. GC38421 Phillyrin (Forsythin) Phillyrin (Forsythin) is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities. Phillyrin (Forsythin)  Chemical Structure
  92. GN10649 Polygalaxanthone III Polygalaxanthone III  Chemical Structure
  93. GC19301 Pradefovir mesylate Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir mesylate  Chemical Structure
  94. GC33862 Pyributicarb (TSH-888) Pyributicarb (TSH-888), a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR). Pyributicarb (TSH-888)  Chemical Structure
  95. GC37061 Quilseconazole Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes. Quilseconazole  Chemical Structure
  96. GC30681 Revexepride Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease. Revexepride  Chemical Structure
  97. GC33780 RG-12525 (NID 525) RG-12525 (NID 525) is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 (NID 525) is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 μM. RG-12525 (NID 525)  Chemical Structure
  98. GC13470 Rhapontigenin inactivator of cytochrome P450 1A1 with antioxidant and anti-cancer activity Rhapontigenin  Chemical Structure
  99. GN10200 Salvianolic acid C Salvianolic acid C  Chemical Structure
  100. GN10425 Schisandrin A Schisandrin A  Chemical Structure
  101. GC37631 Seviteronel Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. Seviteronel  Chemical Structure

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