p450

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).

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

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

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

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

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

Cytochrome P450 2C9 is a cytochrome P-450 subtype that possesses specificity for acidic xenobiotics. It oxidizes a wide range of important clinical drugs under the categories of nonsteroidal anti-inflammatory agents, anticoagulants, hypoglycemic agents, a

Cytochrome P450 CYP1B1 (190-198) [Homo sapiens] is a peptide from Cytochrome c, which is a small heme protein found loosely associated with the inner membrane of the mitochondrion. Cytochromes c from certain eukaryotes, including plants and fungi but not higher animals, contains methylated lysine residues at specific positions1. Cytochrome c is a required cofactor for Apaf-1 function2.

Cytochrome P450 reductase, a NADPH-cytochrome reductase, facilitates an optimal conformation of aromatase for substrate binding [1].

Voxelotor (GBT 440) is a novel hemoglobin S (HbS) polymerization inhibitor primarily used for the treatment of sickle cell disease (SCD) and a cytochrome P450 3A4 inhibitor. Voxelotor targets and covalently binds to the N-terminal valine of the HbS alpha chain, thereby stabilizing sickle cell hemoglobin (HbS).

Cholesterol 24-hydroxylase-IN-1 is an orally active, selective, and potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) that crosses the blood-brain barrier.Cholesterol 24-hydroxylase-IN-1 may be useful in the study of epilepsy-like neurological disorders. Cholesterol 24-hydroxylase-IN-1 is used to study epilepsy-like neurological diseases.

CYP11B2-IN-1 is an effective and selective inhibitor of CYP11B2 with IC50s of 2.3 nM and 142 nM for CYP11B2 and CYP11B1.

BMS-903452 is a potent and selective GPR119 agonist with an EC50 of 14 nM, indicated for the treatment of acute and chronic rodent diabetes. GPR119 is mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. BMS-903452 shows no significant inhibitory effect on 9 cytochrome P450 enzymes (IC50 > 40 μM), does not activate PXR (EC50 > 50 μM), and is not toxic to liver (HEPG2) cell lines.

(-)-Vorozole is an orally active non-steroidal aromatase inhibitor with potency and selectivity. (-)-Vorozole has demonstrated antitumor activity in in vivo experiments. (-)-Vorozole is used in the study of breast cancer.

Vorozole (R83842) is an orally active, potent, and selective nonsteroidal aromatase inhibitor.Vorozole exhibits antitumor activity in vivo and may be used in the study of breast cancer.

Enerisant HCl is a novel potent and selective histamine H3 receptor antagonist, a substrate for P-gp, mediated by cytochrome P450 (CYP) and transporter proteins.

Albaconazole (W-0027) is a small molecule fungal cytochrome P450 family member 51 (fungal CYP51A1) inhibitor. It is used in the treatment of fungal infections, skin and musculoskeletal disorders, and can be used in the study of vulvovaginal candidiasis, Chagas disease and genitourinary disorders.

CYP1B1-IN-1 is a selective and highly potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.

Azalanstat (RS 21607) is an orally available selective mammalian lanosterol 14-alpha-demethylase inhibitor with hypocholesterolemic activity that inhibits cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster livers through inhibition of the cytochrome P450 enzyme, lanosterol 14 alpha demethylase.

MS-PPOH is a potent and selective inhibitor of cytochrome P450 (CYP) epoxygenase, specifically inhibiting CYP2C8 and CYP2C9 with IC50 values of 15 and 11 µM, respectively.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

2-Benzothiazolamine (2-ABT) is a nitrogen-containing heterocyclic compound used as a reaction intermediate in the synthesis of a variety of drugs. It inhibits cytochrome P450 activity and has also shown anti-inflammatory, anticonvulsant and anticancer activities in animal models.

Bifonazole (Bay H-4502) acts to destabilize the fungal cytochrome p450 51 enzyme (also known as Lanosterol 14-alpha-demethylase). It works by inhibiting the production of a substance called ergosterol, which is an essential component of fungal cell membranes. This is vital in the cell membrane structure of the fungus. Its inhibition leads to cell lysis. The disruption in production of ergosterol disrupts the cell membrane and causes holes to appear. The cell membranes of fungi are vital for their survival. They keep unwanted substances from entering the cells and stop the contents of the cells from leaking out.