cyp1

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

CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.

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-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].

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.

CYP17A1-IN-1 (Compound 14) is an inhibitor of CYP17A1 with an IC50 of 26 nM. It exhibits cytotoxicity in androgen-sensitive prostate cancer cells, specifically LNCaP, and hinders the migration of DU-145 cells.

CYP1A1 inhibitor 8a is a potent and selective CYP1A1 inhibitor. It antagonizes B[a]P mediated activation of aromatic hydrocarbon receptor (AhR) in yeast cells, thereby protects human cells from CYP1A1-mediated B[a]P toxicity.

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].

CYP121A1-IN-1 is a potent inhibitor of CYP121A1, demonstrating favorable activity against Mycobacterium tuberculosis (H37Rv MIC 90 ~6.25 μM, ~2.2 μg mL). It significantly reduces mycocyclosin production by blocking the CYP121A1-mediated conversion of cyclo(l-tyrosyl-l-tyrosyl) to mycocyclosin [1].

CYP11B1-IN-2 (compound 7aa) is a selective, orally active inhibitor of CYP11B1 with an IC50 of 9 nM for human CYP11B1 and 25 nM for rat CYP11B1. It can be used to study diseases caused by cortisol overload.

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].

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].

CYP11A1-IN-1 (compound 30) is a selective CYP11A1 enzyme inhibitor with an IC50 of 201-2000 nM, used for studying steroid receptor-mediated diseases, particularly targeting androgen receptors in conditions like prostate cancer [1].

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].

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.

Compound X21 (CYP19A1 CYP11B2-IN-1) is a potent dual inhibitor of aromatase (CYP19A1) and aldosterone synthase (CYP11B2), with IC50 values of 2.3 nM and 29 nM, respectively. It exhibits strong antiproliferative and pro-apoptotic effects on cancer cells. Compound X21 is suitable for breast cancer research purposes [1].

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.

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.

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.

Eupatorin has antiproliferative and antiangiogenic effects. Eupatorin has antiproliferative and cytostatic effects on MDA-MB-468 human breast cancer cells due to CYP1-mediated metabolism. Eupatorin-induced cell death is mediated by both the extrinsic and