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Home >> Signaling Pathways >> Metabolism >> P450

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.

  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. GC12404 (+)-Ketoconazole Potent inhibitor of cytochrome P450c17 (+)-Ketoconazole Chemical Structure
  5. 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
  6. GC14486 (S)-Mephenytoin

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

     (S)-Mephenytoin Chemical Structure
  7. GC33073 1-Ethynylnaphthalene 1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. 1-Ethynylnaphthalene Chemical Structure
  8. GC13836 2,3-dihydrothieno-Thiadiazole Carboxylate CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor 2,3-dihydrothieno-Thiadiazole Carboxylate Chemical Structure
  9. GC12262 2-Phenyl-2-(1-piperidinyl)propane mechanism-based inactivator of human cytochrome P450 (CYP) 2B6 2-Phenyl-2-(1-piperidinyl)propane Chemical Structure
  10. 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
  11. GC65517 4-(Trifluoromethyl)umbelliferone 4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes. 4-(Trifluoromethyl)umbelliferone Chemical Structure
  12. GC11758 4-phenyl-5-methyl-1,2,3-Thiadiazole CYP2B4 and CYP2E1 inhibitor 4-phenyl-5-methyl-1,2,3-Thiadiazole Chemical Structure
  13. 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
  14. 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
  15. GC14781 ABT (1-Aminobenzotriazole) ABT (1-Aminobenzotriazole) is a nonspecific and irreversible inhibitor of cytochrome P450 (P450). ABT (1-Aminobenzotriazole) Chemical Structure
  16. GC35236 Acetylshikonin Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin Chemical Structure
  17. 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
  18. GC65088 Atovaquone-d5 Atovaquone-d5 Chemical Structure
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. GC16256 BVT 948

    PTPs inhibitor,cell-permeable and non-competitve

     BVT 948 Chemical Structure
  25. GC32257 Carbosulfan Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers). Carbosulfan Chemical Structure
  26. GC31464 CDD3505 CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. CDD3505 Chemical Structure
  27. GC31460 CDD3506 CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity. CDD3506 Chemical Structure
  28. GC32991 Cecropin B Cecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic. Cecropin B Chemical Structure
  29. GC38681 Cedrol A sesquiterpene alcohol Cedrol Chemical Structure
  30. GC16751 Chlorzoxazone Muscle-relaxing drug Chlorzoxazone Chemical Structure
  31. GC35692 Chrysosplenetin A flavonoid with diverse biological activities Chrysosplenetin Chemical Structure
  32. GC38758 Clomethiazole Chlormethiazole is an potent and orally active GABAA?agonist. Clomethiazole Chemical Structure
  33. GC41611 Curcumenol Curcumenol is a sesquiterpene that has been found in Curcuma species. Curcumenol Chemical Structure
  34. 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
  35. 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
  36. 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
  37. 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
  38. GC16550 Diosmetin CYP1A1 inhibitor Diosmetin Chemical Structure
  39. 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
  40. 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
  41. GC12892 Doxepin (hydrochloride) histamine, serotonin, adrenergic, and muscarinic receptors antagonist Doxepin (hydrochloride) Chemical Structure
  42. 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
  43. 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
  44. GC12250 Fenofibrate

    PPARα agonist

     Fenofibrate Chemical Structure
  45. GC38623 Fraxinol Fraxinol is isolated from Lobelia chinensis. Fraxinol Chemical Structure
  46. GC32855 Furafylline

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

     Furafylline Chemical Structure
  47. GC14915 Gemfibrozil PPARα activator Gemfibrozil Chemical Structure
  48. 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
  49. GC11540 HET0016 inhibitor of 20-HETE formation HET0016 Chemical Structure
  50. GC16707 Isavuconazole triazole antifungal drug Isavuconazole Chemical Structure
  51. GC36335 Isoglycycoumarin Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis. Isoglycycoumarin Chemical Structure
  52. 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
  53. GC67933 LKY-047 LKY-047 Chemical Structure
  54. 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
  55. GC10198 Memantine hydrochloride NMDA receptor antagonist Memantine hydrochloride Chemical Structure
  56. GC41373 Methysticin Methysticin is a kavalactone isolated from the kava roots. Methysticin Chemical Structure
  57. GC17411 Metyrapone 11-β hydroxylase (CYP11B1) inhibitor Metyrapone Chemical Structure
  58. 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
  59. 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
  60. 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
  61. GC11155 Omeprazole sulfone Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor. Omeprazole sulfone Chemical Structure
  62. 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
  63. GC38421 Phillyrin (Forsythin) Phillyrin (Forsythin) is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities. Phillyrin (Forsythin) Chemical Structure
  64. GC19301 Pradefovir mesylate Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir mesylate Chemical Structure
  65. 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
  66. 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
  67. 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
  68. 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
  69. GC13470 Rhapontigenin inactivator of cytochrome P450 1A1 with antioxidant and anti-cancer activity Rhapontigenin Chemical Structure
  70. 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
  71. GC37632 Seviteronel racemate Seviteronel racemate (VT-464 racemate) is the racemate form of Seviteronel (VT-464), which is a potent CYP17 lyase inhibitor(h-Lyase IC50=nM)inhibition. Seviteronel racemate Chemical Structure
  72. GC16259 SKF 525A (hydrochloride) SKF 525A (hydrochloride) is a Cytochrome P450 inhibitor (IC50 = 19μM). SKF 525A (hydrochloride) Chemical Structure
  73. GC16951 Stiripentol An LDH inhibitor Stiripentol Chemical Structure
  74. GC11638 Sulfaphenazole CYP2C9 inhibitor Sulfaphenazole Chemical Structure
  75. GC37727 Talarozole R enantiomer Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne. Talarozole R enantiomer Chemical Structure
  76. GC32160 Tebuconazole A triazole fungicide Tebuconazole Chemical Structure
  77. GC33833 Tetrahydrocurcumin (HZIV 81-2) Tetrahydrocurcumin (HZIV 81-2) is a Curcuminoid found in turmeric (Curcuma longa) that is produced by the reduction of Curcumin. Tetrahydrocurcumin (HZIV 81-2) Chemical Structure
  78. GC15244 Thienyldecyl Isothiocyanate cytochrome P450 inhibitor Thienyldecyl Isothiocyanate Chemical Structure
  79. GC15445 TMS cytochrome P450 1B1 inhibitor TMS Chemical Structure
  80. GC13362 TOK-001 TOK-001 (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC). TOK-001 Chemical Structure
  81. GC45582 trans-ε-Viniferin ε-Viniferin, the dimer of Resveratrol and isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. trans-ε-Viniferin Chemical Structure
  82. GC17112 Uniconazole cytochrome P450 707As inhibitor Uniconazole Chemical Structure
  83. GC31791 Veledimex (INXN-1001) Veledimex (INXN-1001) (INXN-1001), a synthetic analog of the insect molting hormone ecdysone, is an orally active activator ligand for a proprietary gene therapy promoter system. Veledimex (INXN-1001) Chemical Structure
  84. GC33870 Veledimex racemate (RG-115932 racemate) Veledimex racemate (RG-115932 racemate) (INXN-1001 racemate) is the racemate of veledimex. Veledimex racemate (RG-115932 racemate) Chemical Structure
  85. GC30705 Veledimex S enantiomer (INXN-1001 S enantiome) Veledimex S enantiomer (INXN-1001 S enantiomer) is the S enantiomer of veledimex. Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5. Veledimex S enantiomer (INXN-1001 S enantiome) Chemical Structure
  86. GC15056 β-Nicotyrine

    cytochrome P450 (CYP) isoforms, CYP2A6 and CYP2A13 inhibitor

     β-Nicotyrine Chemical Structure

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