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.
- Cat.No. Product Name Information
-
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.
-
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.
-
GC12404
(+)-Ketoconazole
Potent inhibitor of cytochrome P450c17
-
GC30424
(-)-Cephaeline dihydrochloride (NSC 32944)
(-)-Cephaeline dihydrochloride (NSC 32944) is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
-
GC14486
(S)-Mephenytoin
S-Mephenytoin is an anticonvulsive drug which is metabolized by N-demethylation and 4-hydroxylation .
-
GC33073
1-Ethynylnaphthalene
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
-
GC13836
2,3-dihydrothieno-Thiadiazole Carboxylate
CYP450 enzymes (CYP2E1 and CYP2B4) inhibitor
-
GC12262
2-Phenyl-2-(1-piperidinyl)propane
mechanism-based inactivator of human cytochrome P450 (CYP) 2B6
-
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.
-
GC65517
4-(Trifluoromethyl)umbelliferone
4-(Trifluoromethyl)umbelliferone is fluorescent probe substrate for rat hepatic cytochrome P450 enzymes.
-
GC11758
4-phenyl-5-methyl-1,2,3-Thiadiazole
CYP2B4 and CYP2E1 inhibitor
-
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.
-
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.
-
GC14781
ABT (1-Aminobenzotriazole)
ABT (1-Aminobenzotriazole) is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).
-
GC35236
Acetylshikonin
Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity.
-
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.
-
GC65088
Atovaquone-d5
-
GC34132
Bergamottin (5-Geranoxypsoralen)
Bergamottin (5-Geranoxypsoralen) is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.
-
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.
-
GC65345
BI 653048
BI 653048 is a selective and orally active nonsteroidal?glucocorticoid (GC)?agonist with an IC50 value of 55 nM.
-
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.
-
GC31479
BMS-819881
BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds rat MCHR1 with a Ki of 7 nM.
-
GC16256
BVT 948
PTPs inhibitor,cell-permeable and non-competitve
-
GC32257
Carbosulfan
Carbosulfan inhibited relatively potently CYP3A4 and moderately CYP1A1/2 and CYP2C19 in pooled HLM (human livers).
-
GC31464
CDD3505
CDD3505 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
-
GC31460
CDD3506
CDD3506 is used for elevating high density lipoprotein cholesterol (HDL) by inducing hepatic cytochrome P450IIIA (CYP3A) activity.
-
GC32991
Cecropin B
Cecropin B has high level of antimicrobial activity and is considered as a valuable peptide antibiotic.
-
GC38681
Cedrol
A sesquiterpene alcohol
-
GC16751
Chlorzoxazone
Muscle-relaxing drug
-
GC35692
Chrysosplenetin
A flavonoid with diverse biological activities
-
GC38758
Clomethiazole
Chlormethiazole is an potent and orally active GABAA?agonist.
-
GC41611
Curcumenol
Curcumenol is a sesquiterpene that has been found in Curcuma species.
-
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.
-
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).
-
GC63872
Dagrocorat hydrochloride
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor.
-
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.
-
GC16550
Diosmetin
CYP1A1 inhibitor
-
GC19415
DMU2105
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
-
GC19416
DMU2139
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
-
GC12892
Doxepin (hydrochloride)
histamine, serotonin, adrenergic, and muscarinic receptors antagonist
-
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).
-
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.
-
GC12250
Fenofibrate
PPARα agonist
-
GC38623
Fraxinol
Fraxinol is isolated from Lobelia chinensis.
-
GC32855
Furafylline
Furafylline, as a long-acting replacement for theophylline in the treatment of asthma, is a methylxanthine derivative[1].
-
GC14915
Gemfibrozil
PPARα activator
-
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.
-
GC11540
HET0016
inhibitor of 20-HETE formation
-
GC16707
Isavuconazole
triazole antifungal drug
-
GC36335
Isoglycycoumarin
Isoglycycoumarin is a flavonoid isolated from the roots of Glycyrrhiza uralensis.
-
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.
-
GC67933
LKY-047
-
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.
-
GC10198
Memantine hydrochloride
NMDA receptor antagonist
-
GC41373
Methysticin
Methysticin is a kavalactone isolated from the kava roots.
-
GC17411
Metyrapone
11-β hydroxylase (CYP11B1) inhibitor
-
GC16423
Monoacetylphloroglucinol
Monoacetylphloroglucinol (2,4,6-trihydroxyacetophenone) is the aglycone part of acetophenone glycoside obtained from Curcuma comosa Roxb, with cholesterol-lowering activity.
-
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.
-
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.
-
GC11155
Omeprazole sulfone
Omeprazole sulfone is a metabolite of Omeprazole, which is a proton pump inhibitor.
-
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.
-
GC38421
Phillyrin (Forsythin)
Phillyrin (Forsythin) is isolated from Forsythia suspensa Vahl (Oleaceae), has antibacterial and anti-inflammatory activities.
-
GC19301
Pradefovir mesylate
Pradefovir mesylate is a good substrate for liver CYP3A4.
-
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).
-
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.
-
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.
-
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.
-
GC13470
Rhapontigenin
inactivator of cytochrome P450 1A1 with antioxidant and anti-cancer activity
-
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.
-
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.
-
GC16259
SKF 525A (hydrochloride)
SKF 525A (hydrochloride) is a Cytochrome P450 inhibitor (IC50 = 19μM).
-
GC16951
Stiripentol
An LDH inhibitor
-
GC11638
Sulfaphenazole
CYP2C9 inhibitor
-
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.
-
GC32160
Tebuconazole
A triazole fungicide
-
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.
-
GC15244
Thienyldecyl Isothiocyanate
cytochrome P450 inhibitor
-
GC15445
TMS
cytochrome P450 1B1 inhibitor
-
GC13362
TOK-001
TOK-001 (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC).
-
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.
-
GC17112
Uniconazole
cytochrome P450 707As inhibitor
-
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.
-
GC33870
Veledimex racemate (RG-115932 racemate)
Veledimex racemate (RG-115932 racemate) (INXN-1001 racemate) is the racemate of veledimex.
-
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.
-
GC15056
β-Nicotyrine
cytochrome P450 (CYP) isoforms, CYP2A6 and CYP2A13 inhibitor