cyp1a 1

Diosmetin (Luteolin 4-methyl ether) has been found to act as a weak TrkB receptor agonist.

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).

Iprodione is a fungicide. Iprodione is also used in cannabis testing kits as a component of pesticide mixes.

Tetrahydropiperine (Cosmoperine) is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.

Diflubenzuron (Larvakil) is a benzoyl-urea insecticide, found to be a potent inhibitor of melanosome synthesis in mouse melanoma cells. Diflubenzuron has also been shown to inhibit TCDD-induced CYP1A1 expression in HepG2 cells.

Ellagic Acid Dihydrate inhibit the CYP1A1-dependent activation of benzo[a]pyrene.

1-Ethynylpyrene is an aryl acetylenic inhibitor of CYTP450 1A1 (IC50 = 0.18 μM), 1A2 (IC50 = 0.32 μM), and 2B1 (IC50 = 0.04 μM).

Harman hydrochloride can directly induce CYP1A1 gene expression in an AhR-dependent manner and may represent a novel mechanism by which harman promotes mutagenicity, co-mutagenicity and carcinogenicity.

BAY 2416964 is a small molecule inhibitor that selectively targets aromatic receptor (AhR) with an IC50 of 341 nM and is commonly used in cancer immunotherapy research.

Olivetol (5-n-Amylresorcinol) (5-pentylresorcinol, 5-pentyl-1,3-benzenediol) is an organic compound found in certain species of lichen; it is also a precursor in various syntheses of tetrahydrocannabinol. Olivetol has an antioxidant effect.

Rhapontigenin (Protigenin) is a mechanism-based, selective inactivator of cytochrome P450 1A1 (IC50: 400 nM), an aryl hydrocarbon hydroxylase which activates polycyclic aromatic hydrocarbons that act as procarcinogens. Rhapontigenin is a natural analog of resveratrol with antioxidant and anti-cancer activity. At higher concentrations, rhapontigenin inhibits the proliferation of HL-60R and HepG2 cancer cell lines (IC50: 48 μM).

1. Bergamottin (5-Geranoxypsoralen) can significantly reduce blood glucose and increase glucose tolerance and insulin sensitivity in KK-A^ydiabetic mice.

Visnagin has acute hypotensive, anti-inflammatory, and neuroprotective effects, it protects against doxorubicin-induced cardiomyopathy through modulation of mitochondrial malate dehydrogenase.

Chalepensin, a furanocoumarin isolated from the rutaceae plant Ruta chalepensis L., is a selective CYP2A6 inhibitor, inhibiting CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4.Chalepensin exhibits Chalepensin j has antiprotozoal activity and inhibits methicillin-resistant Staphylococcus aureus (MRSA) with MIC values in the range of 32-128 μg/mL.

Methysticin, a major kavalactone extracted from kava, can induce CYP1A1.

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.

BAY-218 is an aryl hydrocarbon receptor (AHR) antagonist with IC50 of 39.9 nM in the human glioblastoma U87 cell line. BAY-218 inhibition of AhR stimulates pro-inflammatory monocyte and T cell responses in vitro and drives anti-tumor immune responses, leading to reduced tumor growth in vivo.

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

Antitumor agent-87 is a potent compound exhibiting high antitumoral activity, with a Ki value of 0.23 µM for CYP1A1. It demonstrates antiproliferative effects and induces cell cycle arrest at the G2/M phase, underscoring its effectiveness as an antitumor agent.

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.

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.

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

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].

Antitumor agent-88, a competitive inhibitor of CYP1A1 (K i: 1.4 μM), demonstrates significant antimitotic activity by arresting cells in the G2/M phase and disrupting the microtubule network and cytoskeleton in CYP1A1-expressing breast cancer cells.