cyp1

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

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.

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.

CYP19A1-IN-1 (Compound 9) is an inhibitor of CYP19A1 with an IC50 value of 271 nM. It functions by binding to CYP19A1, thereby inhibiting its activity in converting androgens to estrogens. CYP19A1-IN-1 is applicable in research related to estrogen-dependent breast cancer and other sex hormone-related conditions.

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.

CYP17A1/HDAC6-IN-1 (compound 12) is a potent inhibitor of CYP17A1 and HDAC6, with IC50 values of 0.284 μM and 0.6015 μM, respectively. It exhibits antitumor activity.

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.

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.

CYP11B2-IN-3 (compound 32) is an orally active and selective inhibitor of CYP11B2, with IC50 values of 12.92 nM for CYP11B2 and 2341 nM for CYP11B1. It is applicable in hypertension research.

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.

CYP1A1-IN-1 (Compound 47) is a small molecule inhibitor of cytochrome P450 1A1 (CYP1A1). It reduces the bacterial load of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii by enhancing macrophage phagocytosis. CYP1A1-IN-1 shows potential for research in sepsis caused by multi-drug resistant (MDR) bacteria.

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).

CYP11A1-IN-2 (Compound 61) is a selective inhibitor of cholesterol side-chain cleavage enzyme (CYP11A1). This compound has the ability to inhibit steroid biosynthesis and may be utilized in research on steroid hormone-dependent cancers, such as prostate cancer.

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].

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.