cyp1b1

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

CYP1B1-IN-5 is a selective and potent cytochrome P450 1B1 (CYP1B1) inhibitor with an IC50 of 4.7 nM.CYP1B1-IN-5 can be used for the study of metabolism-related diseases.

CYP1B1-IN-4, a 2,4-diarylthiazole compound, exhibits selective inhibition of CYP1B1 (IC50=0.2 nM), demonstrating minimal cytotoxicity and high stability in human and rat liver microsomes [1].

DMU2139 is a specific CYP1B1 inhibitor (CYP1B1 and CYP1A1 with IC50 of 9 nM and 795 nM, respectively).

PROTAC CYP1B1 degrader-2 (compound PV2), a VHL (von Hippel - Landau) E3 ligase-based degrader of CYP1B1, exhibits a DC50 of 1.0 nM after 24 hours in A549 Taxol cells. Furthermore, it effectively inhibits the growth, migration, and invasion of A549 Taxol cells.

PROTAC CYP1B1 Degrader-1 (Compound 6C), an α-naphthoflavone chimera derivative, effectively targets and degrades cytochrome P450 (CYP) 1B1 to overcome agent resistance, displaying half-maximal inhibitory concentrations (IC50s) of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2. This compound is suitable for investigating prostate cancer characterized by overexpression of CYP1B1 [1].

CYP1B1-IN-2 (compound 9j) is a highly potent and selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 value of 0.52 nM [1].

CYP1B1-IN-7 is a selective and potent CYP1B1 inhibitor showing cytotoxic effects in docetaxel-resistant CYP1B1 overexpressing MCF-7 cell lines, and can be used in synergistic treatment of cancer with anticancer compounds.

CYP1B1 Ligand 3 (Compound A1) functions as a selective inhibitor of the cytochrome P450 enzyme CYP1B1, with an IC50 of 11.9 nM. It is also utilized in the synthesis of PROTAC CYP1B1 Degrader-2.

CYP1B1-IN-3 is a potent, selective inhibitor of CYP1B1, exhibiting IC50 values of 6.6 nM for CYP1B1, 347.3 nM for CYP1A1, and >10000 nM for CYP1A2. It also impedes cell migration and invasion, and inhibits the P-gp, AKT ERK, FAK SRC, and EMT pathways [1].

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.

hCYP1B1-IN-1 (compound B18) is an hCYP1B1 inhibitor with an IC50 of 3.6 nM, acting as an Aryl Hydrocarbon Receptor antagonist. It demonstrates favorable metabolic stability and good cell permeability, and inhibits the migration of MCF-7 cells [1].

1-Ethynylnaphthalene [1-EN] is a selective inhibitor of cytochrome P450 IB1 (CYP1B1).

Alizarin (Mordant Red 11), a red dye derived from the roots of plants of the madder genus, inhibits P450 isoform CYP1A1( IC50 = 6.2 μM), CYP1A2 (IC50 =10.0 μM )and CYP1B1(IC50 = 2.7 μM).

Dolutegravir M1 is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed primarily by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1. 1.Zhu, J., Wang, P., Li, F., et al.CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitorBiochem. Pharmacol.158174-184(2018)

TMS (2,3',4,5'-Tetramethoxystilbene) is a very selective and potent competitive inhibitor of P450 1B1 (CYP1A1).

1,2,3,4,7,8-Hexachlorodibenzofuran (1,2,3,4,7,8-HxCDF) enhances the expression of CYP1A1, CYP1B1, and aryl hydrocarbon receptor repressor (AhRR) genes in human peripheral blood lymphocytes (PBL). It can activate ethoxyresorufin-O-deethylase (EROD), with a BMR20TCDD within the range of 0.115-0.143 nM, corresponding to 20% of the maximum response induced by TCDD.

1,2,3,4,7,8,9-Heptachlorodibenzofuran (1,2,3,4,7,8,9-HpCDF) is a chemical compound known for inducing the expression of CYP1A1 and CYP1B1 genes in human peripheral blood lymphocytes, while also enhancing the expression of the aromatic hydrocarbon receptor repressor (AhRR). In isolated human peripheral blood lymphocytes, it boosts ethoxyresorufin-O-deethylase (EROD) activity—a marker for CYP1A1 activity—in a concentration-dependent manner. Additionally, 1,2,3,4,7,8,9-HpCDF exhibits immunosuppressive properties, reducing the number of plaque-forming cells in mouse spleens and increasing aromatic hydrocarbon hydroxylase (AHH) activity in the liver microsomes of mice injected with sheep red blood cells. This compound is pertinent to research in the fields of immunology, metabolic diseases, and environmental toxicology.

ε-Viniferin (epsilon-Viniferin) a dimer of resveratrol, shows the inhibitory effects of epsilon-viniferin on human CYP1A1, CYP1A2, CYP1B1, CYP2A6, CYP2B6, CYP2E1, CYP3A4 and CYP4A activities.

DMU2105 is a specific CYP1B1 inhibitor(CYP1B1 and CYP1A1 with IC50 of 10 nM and 742 nM, respectively)