Cytochrome P450

Cat. No.

A69817

CAS No.

2280834-99-1

CYP4A11/CYP4F2-IN-2

CYP4A11/CYP4F2-IN-2 is a selective inhibitor of CYP4A11 and CYP4F2, exhibiting IC50 values of 120 nM and 220 nM, respectively. This compound effectively inhibits the production of 20-HETE in rat kidney models, demonstrating potential in research related to diabetic nephropathy and autosomal dominant polycystic kidney disease. Its oral bioavailability makes it a valuable tool for exploring the therapeutic effects of CYP4A11 and CYP4F2 inhibition in relevant biological conditions.

Cat. No.

A69820

CAS No.

2562383-94-0

CYP3A4-IN-2

CYP3A4-IN-2 is a selective inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 0.055 μM. As a ritonavir analogue, it possesses enhanced hydrophobicity in the R2 side group, resulting in a more potent inhibitory effect than ritonavir. This reagent is applicable in research focused on antiviral therapies and immunosuppressive mechanisms.

Cat. No.

A69822

CAS No.

132042-69-4

(-)-Vorozole

(-)-Vorozole is a selective inhibitor of cytochrome P450, specifically targeting aromatase. This non-steroidal compound exhibits significant antitumor activity in vivo and is primarily utilized in breast cancer research. Its potent inhibitory properties make it a valuable tool for investigating estrogen synthesis and its implications in various malignancies.

Cat. No.

A69823

CAS No.

1422527-87-4

CYP1A1-IN-2

CYP1A1-IN-2 is a competitive inhibitor of CYP1A1 with a Ki value of 1.4 μM. This compound demonstrates significant antimitotic activity by effectively arresting cells in the G2/M phase of the cell cycle. Furthermore, CYP1A1-IN-2 disrupts microtubule integrity and the cytoskeletal structure in breast cancer cells that express CYP1A1, making it a valuable tool for studies on cancer biology and therapeutic resistance.

Cat. No.

A69826

CAS No.

3057862-18-4

CYP11A1-IN-2

CYP11A1-IN-2 is a selective inhibitor of the cholesterol side-chain cleavage enzyme CYP11A1. This compound effectively inhibits steroid biosynthesis, making it a valuable tool for investigating steroid hormone-dependent cancers, including prostate cancer. Its application in research enables the exploration of novel therapeutic strategies targeting steroid pathways.

Cat. No.

A69828

CAS No.

2760611-38-7

CYP4Z1-IN-1

CYP4Z1-IN-1 is a potent inhibitor of the cytochrome P450 enzyme CYP4Z1, exhibiting an IC50 of 41.8 nM. This compound effectively reduces the expression of cancer stem cell (CSC) markers associated with breast cancer, as well as inhibiting spheroid formation, metastatic potential, and tumor initiation capabilities in both in vitro and in vivo models. Its application in cancer research enhances understanding of CSC biology and potential therapeutic avenues targeting CYP4Z1.

Cat. No.

A69829

CAS No.

1713317-28-2

GW273297X

Synonyms: G297X

GW273297X is a selective inhibitor of CYP27A1, a key enzyme involved in cholesterol metabolism. This compound effectively reduces the concentration of 27-hydroxycholesterol (27HC) in E0771 tumor models in APOE3 mice. GW273297X serves as a valuable tool for investigating the role of CYP27A1 in breast cancer research and its potential impact on tumor progression and metabolism.

Cat. No.

A69830

CAS No.

302-33-0

Proadifen

Proadifen is a selective inhibitor of cytochrome P450 enzymes, impacting the metabolic activity of various substrates. Its inhibitory action can modulate the excitability of catecholamine-secreting neurons, potentially leading to differential effects across distinct brain regions. Proadifen is utilized in research to investigate the role of cytochrome P450 in neurotransmitter regulation and neuropharmacology.

Cat. No.

A69833

CAS No.

2404-87-7

3-Phenylthiophene

3-Phenylthiophene is a selective inhibitor of CYP2A6 with a Ki value of 3.3 μM. It demonstrates minimal inhibition of other cytochrome P450 enzymes, including CYP2E1 (Ki 9.7 μM), CYP2B6 (Ki 14 μM), CYP2C9 (Ki 112 μM), and CYP2C19 (Ki 107 μM), while showing no significant activity against CYP3A4 and CYP2D6. This compound is valuable for research applications aimed at understanding smoking cessation mechanisms and the metabolism of nicotine.

Cat. No.

A69835

CAS No.

2562384-19-2

CYP3A4-IN-3

CYP3A4-IN-3 is a potent and selective inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 0.075 μM. This compound, a modified analogue of ritonavir, demonstrates significantly enhanced inhibitory efficacy compared to its predecessor. CYP3A4-IN-3 is primarily utilized in antiviral research and immunosuppression studies, serving as a valuable tool for investigating drug metabolism and therapeutic interventions.

Cat. No.

A69838

CAS No.

727730-24-7

CYP1B1-IN-2

CYP1B1-IN-2 is a highly potent and selective inhibitor of cytochrome P450 1B1 (CYP1B1), exhibiting an IC50 of 0.52 nM. This compound is valuable for research exploring the role of CYP1B1 in various biological processes, including cancer metabolism and drug metabolism. Its specificity makes it a useful tool for studying CYP1B1-related pathways and potential therapeutic applications.

Cat. No.

A69842

CAS No.

101236-51-5

Kushenol M

Kushenol M is a flavonoid derived from Sophora flavescens, functioning primarily as a cytochrome P450 (CYP) inhibitor. It exhibits potent inhibitory activity, with an IC50 value of 1.29 μM specifically for CYP3A4 in human liver microsomes. This compound is valuable for research involving drug metabolism and pharmacokinetics, as well as studies assessing the interactions and regulation of CYP enzymes.

Cat. No.

A69844

CAS No.

176442-56-1

CYP1B1-IN-5

CYP1B1-IN-5 is a highly potent and selective inhibitor of cytochrome P450 1B1 (CYP1B1), exhibiting an IC50 of 4.7 nM. This compound is valuable for research applications aimed at understanding the role of CYP1B1 in various biological processes, including cancer metabolism and toxicity. Its specificity and efficacy make it an important tool for exploring CYP1B1's contributions to disease mechanisms and potential therapeutic interventions.

Cat. No.

A69845

CAS No.

1613481-52-9

Cholesterol 24-hydroxylase-IN-2

Cholesterol 24-hydroxylase-IN-2 is a potent inhibitor of cholesterol 24-hydroxylase (CH24H or CYP46A1) with an IC50 value of 5.4 nM. This compound serves as a valuable tool for studying cholesterol metabolism and is particularly useful in imaging studies involving CH24H in mammalian systems. Its ability to selectively inhibit CH24H facilitates research on neurodegenerative diseases and related metabolic pathways.

Cat. No.

A69847

CAS No.

889959-22-2

CYP19A1-IN-1

CYP19A1-IN-1 is a selective inhibitor of CYP19A1, exhibiting an IC50 of 271 nM. By binding to CYP19A1, it effectively inhibits the conversion of androgens to estrogens. This reagent is valuable for research applications focused on estrogen-dependent diseases, including breast cancer, enabling studies on hormone regulation and potential therapeutic interventions.

Cat. No.

A69854

CAS No.

504-84-7

Erysolin

Erysolin is a selective CYP1A inhibitor known for its antitumor properties. It effectively reduces benzo(a)pyrene-induced genotoxicity, making it valuable for research into the mechanisms of chemical carcinogenesis. Erysolin's ability to modulate CYP1A activity may provide insights into the metabolic pathways involved in drug metabolism and toxicity.

Cat. No.

A69863

CAS No.

1429329-63-4

ASN-001

ASN-001 is an orally active CYP-17A1 lyase inhibitor that selectively targets testosterone synthesis. This compound exhibits notable anticancer activity, particularly in the context of prostate cancer research. Its specific mechanism of action makes ASN-001 a valuable tool for studying androgen-dependent malignancies and developing treatment strategies.

Cat. No.

A69864

CAS No.

2771297-34-6

CYP3A4-IN-1

CYP3A4-IN-1 is a potent inhibitor of cytochrome P450 3A4 (CYP3A4), demonstrating an inhibition constant (IC50) of 0.085 µM. This compound is essential for studies involving drug metabolism and pharmacokinetics, particularly in the context of identifying potential drug-drug interactions. Its use can facilitate research in pharmacology and toxicology by evaluating the effects of CYP3A4 inhibition on various therapeutic agents.

Cat. No.

A69865

CAS No.

264234-05-1

(R)-6',7'-Dihydroxybergamottin

Synonyms: (R)-6′,7′-DHB

(R)-6',7'-Dihydroxybergamottin is a competitive inhibitor of cytochrome P450 1A1 (CYP1A1) with inhibition constants (Kis) of 55 μM for human CYP1A1 and 1.72 μM for rat CYP1A1. This compound is primarily utilized in cancer research, offering insights into CYP1A1's role in cancer biology and pharmacology. Its inhibitory properties make it a valuable tool for studying CYP1A1-related pathways and cancer metabolism.

Cat. No.

A69873

CAS No.

2872575-51-2

CYP1B1-IN-3

CYP1B1-IN-3 is a selective inhibitor of CYP1B1, exhibiting an IC50 of 6.6 nM for this target while demonstrating minimal activity against CYP1A1 and CYP1A2 with IC50 values of 347.3 nM and >10000 nM, respectively. This compound effectively inhibits cell migration and invasion, along with modulation of critical signaling pathways, including P-glycoprotein, AKT/ERK, FAK/SRC, and epithelial-mesenchymal transition (EMT). CYP1B1-IN-3 serves as a valuable tool for research applications focusing on cancer metastasis and the underlying mechanisms of CYP1B1 activity in various biological systems.

Cat. No.

A69876

CAS No.

105-21-5

Gamma-heptalactone

Synonyms: γ-Oenantholacton

Gamma-heptalactone is a selective inhibitor of cytochrome P450 2B6 (CYP2B6), exhibiting an IC50 of 2400 μM. This compound is valuable for studies investigating the metabolism of drugs by CYP2B6 and can aid in understanding the pharmacokinetics of various therapeutic agents. Its inhibitory properties make it a useful tool for exploring drug-drug interactions and metabolic pathways involved in the biotransformation of xenobiotics.

Cat. No.

A69881

CAS No.

573-98-8

1,2-Dimethylnaphthalene

1,2-Dimethylnaphthalene is identified as a potent inhibitor of CYP1A2, exhibiting an IC₅₀ of 5.5 μM and a corresponding pIC₅₀ of 5.26. This compound plays a significant role in studies focused on drug metabolism and enzyme inhibition. It is valuable for understanding the modulation of CYP450 enzymes in various physiological and pathological conditions.

Cat. No.

A69885

CAS No.

54984-93-9

DL-Acetylshikonin

DL-Acetylshikonin is a reversible, non-selective inhibitor of cytochrome P450 enzymes, demonstrating IC50 values between 1.4 and 4.0 μM. This compound exhibits notable anti-cancer and anti-inflammatory activities, making it a valuable tool in cancer research and studies focused on inflammation pathways. Its inhibition of cytochrome P450 provides insights into drug metabolism and therapeutic strategies.

Cat. No.

A69886

CAS No.

108210-73-7

Bifeprofen

Bifeprofen is a selective inhibitor of cytochrome P450 2C9 (CYP2C9), exhibiting dose-dependent inhibition with an IC50 value of 75 µM. This compound is utilized in pharmacological research to study drug metabolism and interactions mediated by CYP2C9. Its application may extend to understanding the implications of CYP2C9 inhibition in clinical settings, providing insights into personalized medicine and therapy optimization.

Cat. No.

A69891

CAS No.

612-58-8

3-Methylquinoline

3-Methylquinoline is a selective inhibitor of cytochrome P450 1A2 (CYP1A2) with an IC50 value of 13 μM. This compound is known to decrease the metabolic clearance of substrates processed by CYP1A2, thereby enhancing the pharmacological effects of these drugs. Additionally, 3-Methylquinoline is capable of inhibiting the activation of certain carcinogenic precursors, making it a valuable tool in cancer research and drug metabolism studies.