p450

Climbazole (BAY-e 6975) is a broad-spectrum imidazole antifungal agent with anti-dandruff properties.

Uniconazole is a plant growth regulator that inhibit cytochrome P450 707As (Ki=68 nM). CYP707As is a major ABA catabolic enzyme that catabolize Abscisic acid, accordingly suppress gibberellin and sterol biosynthesis.

Tienilic Acid is a uricosuric diuretic with certain hepatotoxicity

1-Ethynylpyrene is an aryl acetylenic inhibitor of CYTP450 1A1 (IC50 = 0.18 μM), 1A2 (IC50 = 0.32 μM), and 2B1 (IC50 = 0.04 μM).

LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes. LY 43578 can be used to study neurological and cardiovascular diseases.

GSK-25 maintains good selectivity against a panel of 31 kinases, as well as RSK1 and p70S6K (RSK1 IC50 of 398 nM, p70S6K IC50 of 1000nM), and a dramatically improved P450 profile (>2.2 uM at all isozymes tested).

4'-Methylchrysoeriol is a potent inhibitor of cytochrome P450 enzymes (IC50: 19 nM for human P450 1B1-dependent EROD).

BVT948 is a protein tyrosine phosphatase (PTP) inhibitor that also inhibits lysine methyltransferase SETD8 (KMT5A) and various cytochrome P450 (P450) isoforms.

Norfluoxetine Hydrochloride (Norfluoxetine HCl) is an active metabolite of fluoxetine. Fluoxetine is an antidepressant drug.

(S)-Mephenytoin ((+)-Mephenytoin) is an anticonvulsant that serves as a substrate of the cytochrome P450 (CYP) isoform CYP2C19 and is used to analyze cytochrome P450 metabolism.

Ginsenoside Rd (Gypenoside VIII) may have properties that inhibit or prevent the growth of tumors.

Choline Fenofibrate (Trilipix) is a choline formulation of fenofibrate, a synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity.

Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin, a P450 1A1 inhibitor, which may be used to prevent cancer.

β-Amyrin (beta-Amyrin) has antiviral, hepatoprotective, antinociceptive, anti-inflammatory

Seneciphylline, one of the hepatotoxic pyrolizidine alkaloids, has mutagenic activity in Drosophila and their transfer into rat milk.Seneciphylline can significantly increased the activities of epoxide hydrase and glutathione-S-transferase but cause reduc

8-Geranyloxypsoralen inhibits α2-secretase (BACE1) activity in non-competitive manner, with the IC(50) values <25.0 μM, it can induce vasorelaxation on rat arterial tissues. 8-Geranyloxypsoralen possesses nematicidal activities, the median lethal concentrations (LC(50)) is 188.3 mg/ L against B. xylophilus and is 117.5 mg/L against P. redivivus.

Alpha-Amyrin (alpha-Amyrine) is an inhibitor of trypsin and chymotrypsin with antineoplastic effects. alpha-Amyrin can be used in studies about acting as a hepatomodulatory.

α-Viniferin known as 2-arylbenzofuran flavonoids, that are inhibitors of prostaglandin H2 synthetase. α-Viniferin has anti-Alzheimer's disease, anti-tuberculosis, anti-tumor, anti-inflammation, anti-diabetes and other pharmacological activitie

Ayanin has vasorelaxant activity, it also may have the potential for use in treating allergic asthma.The IC(50) value of Ayanin (quercetin-3,7,4'-O-trimethylether) is 2.2microM for inhibiting interleukin (IL)-4 production from purified basophils.

Chamaechromone is a natural product isolated from the roots of Stellera chamaejasme L.. Chamaechromone has anti-HBV and insecticidal activity.

Corydalmine exhibits antibacterial activities against Staphylococcus aureus and methicillin-resistant S. aureus strains.1-Corydalmine significantly inhibits spore germination of all the fungi at 100 to 1500 ppm. l-Corydalmine also exhibits potent analgesic activity in preclinical models, it is under development as an oral analgesic agent.

Friedelin possesses antioxidant, gastroprotective, anti-diarrhoeal, liver protective, anti-inflammatory, analgesic and antipyretic activities.

5-Methylcytosine is a methylated nucleotide base found in eukaryotic DNA. It is an epigenetic modification formed by the action of DNA methyltransferases.

Glycycoumarin is an estrogen agonist, it shows moderate inhibitory effects against CYP1A2 and CYP2B6.