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-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.

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.

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.

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).

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

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

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 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.

CYP1B1-IN-6 (compound 19) is a fluorescent molecular probe that inhibits the activity of CYP1B1. It enables the identification of tumor sites through fluorescence and photoacoustic imaging modes.

CYP1B1-IN-8 (Compound 14b) is a CYP1B1 inhibitor with an IC50 of 4.14 × 10⁻⁵ nM. It reduces the resistance of A549 cells to paclitaxel and inhibits cell migration and invasion.

CYP1B1-IN-9 is a highly selective and competitive CYP1B1 inhibitor, with IC50 values of 1.48 nM for CYP1B1, and greater than 100 μM and 80 μM for CYP1A1 and CYP1A2, respectively. This compound effectively inhibits the migration and invasion of A549/T cells, offers the potential to resensitize paclitaxel-resistant cells, and exhibits good metabolic stability and safety, as well as favorable pharmacokinetic properties. CYP1B1-IN-9 is applicable in research on tumor resistance.

CYP1B1-IN-10 (Compound 15C) is a highly selective inhibitor of human cytochrome P450 1B1 (hCYP1B1) with an IC50 value of 0.11 μM. It shows promise for use in research focused on hormone-dependent tumors, including breast and ovarian cancers.

CYP1B1-IN-11 (Compound M2) is a selective CYP1B1 inhibitor with an IC50 of 0.00605 pM. It effectively reverses DMBA-induced paclitaxel resistance and inhibits the invasion and migration of tumor cells. CYP1B1-IN-11 is applicable for research in tumor resistance.

CYP1B1-IN-12 is a selective inhibitor of cytochrome P4501B1 (CYP1B1) with an IC50 value of 6.05 nM. It demonstrates exceptional selectivity, being over 1,600 times more selective for CYP1B1 compared to CYP1A1 and over 16,000 times compared to CYP1A2. CYP1B1-IN-12 enhances Paclitaxel-mediated apoptosis and restores sensitivity of A549/Tax cells to Paclitaxel. It also inhibits epithelial-mesenchymal transition, reducing cell migration and invasion. CYP1B1-IN-12 is applicable in cancer research, such as non-small cell lung cancer (NSCLC).

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-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].

CYP1B1 ligand 2 is the target protein ligand for PROTACCYP1B1 degrader-2. It is applicable in lung cancer research.

hCYP1B1-IN-2 (compound 3n) is a potent inhibitor of the human enzyme cytochrome P450 1B1 (hCYP1B1). It exhibits strong anti-hCYP1B1 activity with an IC50 of 0.040 nM and can also block AhR transcriptional activity. hCYP1B1-IN-2 effectively inhibits hCYP1B1 through a mixed inhibition mode with a Ki value of 21.71 pM.

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].

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

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