Cytochrome P450

Cat. No.

A69706

CAS No.

93879-40-4

(±)-N-3-Benzylnirvanol

(±)-N-3-Benzylnirvanol acts as an inhibitor of the cytochrome P450 enzyme CYP2C19. This racemic mixture, comprised of both (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol, exhibits potent inhibitory activity with Ki values of 0.25 μM and 5.3 μM, respectively, for the respective enantiomers. It is valuable in pharmacological research aimed at understanding drug metabolism and potential drug-drug interactions involving CYP2C19.

Cat. No.

A69714

CAS No.

92321-29-4

2-Phenyl-2-(1-piperidinyl)propane

2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible inhibitor of the human cytochrome P450 enzyme CYP2B6, displaying an IC50 value of 5.1 μM and a Ki of 5.6. In addition to its primary activity, this compound also moderately inhibits CYP2D6 and CYP3A, with IC50 values of 74 μM and 200 μM, respectively. This reagent is pertinent for research into drug metabolism and interactions involving CYP2B6 and other related P450 enzymes.

Cat. No.

A69719

CAS No.

2685779-55-7

CYP1B1-IN-4

CYP1B1-IN-4 is a selective CYP1B1 inhibitor, demonstrating a potent inhibitory activity with an IC50 value of 0.2 nM. This compound exhibits low cytotoxicity and maintains high stability in both human and rat liver microsomes, making it suitable for pharmacological studies. Its selectivity and stability position CYP1B1-IN-4 as a valuable tool for research into CYP1B1-related biological pathways and diseases.

Cat. No.

A69726

CAS No.

4846-19-9

N-Nornuciferine

N-Nornuciferine is an aporphine alkaloid derived from lotus leaves that selectively inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 3.76 μM and a Ki of 2.34 μM. This compound plays an important role in pharmacological research by modulating drug metabolism and interactions. Its potency as a CYP2D6 inhibitor makes it a valuable tool for studies investigating drug efficacy and toxicity related to cytochrome P450 enzymatic pathways.

Cat. No.

A69728

CAS No.

2126874-77-7

TP0472993

TP0472993 is a potent and orally active dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 140 nM and 40 nM, respectively. This compound is valuable for investigating the role of these enzymes in renal diseases, contributing to a deeper understanding of their biological functions and potential therapeutic implications. Its selective inhibition profile makes TP0472993 a useful tool for studying the pharmacological effects related to cytochrome P450-mediated pathways.

Cat. No.

A69731

CAS No.

937263-81-5

ONT-993

Synonyms: AR 00440993

ONT-993 is a hydroxylated metabolite that primarily inhibits the cytochrome P450 enzyme CYP2D6, with an IC50 value of 7.9 µM. Additionally, ONT-993 induces metabolism-dependent inactivation of CYP3A, characterized by a KI of 1.6 µM. This compound is useful in research applications focused on drug metabolism and pharmacokinetics, particularly regarding interactions involving CYP450 enzymes.

Cat. No.

A69733

CAS No.

2744168-51-0

CYP11A1-IN-1

CYP11A1-IN-1 is an inhibitor of cytochrome P450 11A1 (CYP11A1), exhibiting an IC50 range of 201-2000 nM. This compound is valuable for research focusing on steroid hormone synthesis and the role of androgens in diseases such as prostate cancer. It offers potential applications in studies related to androgen receptor-dependent pathways and their therapeutic implications.

Cat. No.

A69734

CAS No.

186299-00-3

hCYP3A4 Fluorogenic substrate 1

hCYP3A4 Fluorogenic Substrate 1 is a potent substrate designed for human cytochrome P450 3A4 (hCYP3A4), exhibiting a Km value of 0.36 μM. This substrate is valuable for investigating hCYP3A4-mediated biotransformation processes and can be utilized in both cellular and in vivo imaging studies to monitor enzyme activity. Its fluorogenic properties facilitate real-time observation of metabolic activity, aiding in drug metabolism and pharmacokinetic research.

Cat. No.

A69735

CAS No.

80434-32-8

1β-Hydroxydeoxycholic acid

Synonyms: 1β-OH-DCA

1β-Hydroxydeoxycholic acid (1β-OH-DCA) is a secondary bile acid and a recognized biomarker for the CYP3A enzyme family. It is primarily generated through the metabolism of deoxycholic acid via CYP3A4 and CYP3A7 employing recombinant human CYP450 enzymes. This compound serves as an important tool in pharmacokinetic studies and the evaluation of drug metabolism, facilitating research in drug interactions and personalized medicine involving CYP3A activity.

Cat. No.

A69738

CAS No.

34993-56-1

1-Ethynylpyrene

1-Ethynylpyrene is a potent inhibitor of cytochrome P450 enzymes, specifically P450 1A1, 1A2, and 2B1, displaying IC50 values of 0.18, 0.32, and 0.04 μM, respectively. This compound also serves as a versatile click chemistry reagent, featuring an alkyne group that facilitates copper-catalyzed azide-alkyne cycloaddition (CuAAc) for bioconjugation applications. Its unique properties make it valuable for studies involving drug metabolism and chemical biology.

Cat. No.

A69741

CAS No.

877-43-0

2,6-Dimethylquinoline

2,6-Dimethylquinoline is a selective inhibitor of CYP1A2, exhibiting an IC50 of 3.3 µM. Additionally, it shows inhibitory activity towards CYP2B6 with an IC50 of 480 µM. This compound, derived from the roots of Peucedanum praeruptorum, serves as a valuable tool for research into drug metabolism and pharmacokinetics, particularly in studies exploring cytochrome P450 enzyme modulation.

Cat. No.

A69743

CAS No.

7437-55-0

8-Geranyloxypsoralen

8-Geranyloxypsoralen is a furanocoumarin that serves as a potent inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting an IC50 value of 3.93 μM. This compound is commonly utilized in research to explore drug metabolism and potential interactions involving CYP3A4, which plays a critical role in the biotransformation of numerous therapeutic agents. The inhibition of CYP3A4 by 8-Geranyloxypsoralen can facilitate the study of pharmacokinetics and enzyme regulation in cellular models.

Cat. No.

A69745

CAS No.

1260006-20-9

Lapiteronel

Synonyms: CFG920

Lapiteronel is a nonsteroidal, orally active inhibitor of CYP17 and CYP11B2, functioning as a reversible dual inhibitor. This compound exhibits significant biological activity in the modulation of steroid hormone synthesis, making it a valuable tool for research in metastatic castration-resistant prostate cancer. Its role in inhibiting critical enzymatic pathways positions Lapiteronel as a potential therapeutic agent in advancing cancer treatment studies.

Cat. No.

A69746

CAS No.

88511-35-7

1-(Isothiazol-3-yl)ethan-1-one

Synonyms: 1-(Isothiazol-3-yl)ethanone

1-(Isothiazol-3-yl)ethan-1-one is a selective inhibitor of CYP2E1, an enzyme involved in the metabolism of various xenobiotics and endogenous compounds. This compound has demonstrated potential in modulating pathways relevant to oxidative stress and inflammation. Its applications extend to research on conditions such as rheumatoid arthritis and sepsis, providing insights into therapeutic strategies targeting these diseases.

Cat. No.

A69748

CAS No.

486-28-2

Fraxinol

Fraxinol is a potent inhibitor of cytochrome P450 enzymes, primarily investigated for its role in drug metabolism and biotransformation. This compound, isolated from Lobelia chinensis, has demonstrated significant biological activity, making it relevant in studies focusing on pharmacokinetics and potential drug interactions. Fraxinol can be utilized in research aimed at understanding the metabolic pathways and toxicity profiles of various pharmaceuticals.

Cat. No.

A69750

CAS No.

1375603-38-5

Seviteronel (R enantiomer)

Synonyms: VT-464 (R enantiomer)

Seviteronel (R enantiomer) is a potent inhibitor of CYP17 lyase, with an h-Lyase IC50 value of 69 nM. This compound specifically targets the cytochrome P450 17A1 enzyme, crucial in steroidogenesis, and has applications in research focused on hormone-dependent cancers. Its efficacy in inhibiting steroid biosynthesis makes it a valuable reagent for studies investigating hormonal modulation and therapeutic interventions.

Cat. No.

A69751

CAS No.

65823-65-6

CYP1B1 ligand 3

CYP1B1 ligand 3 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 of 11.9 nM. This compound is significant for research involving the modulation of CYP1B1 activity and serves as a valuable tool in the development of PROTAC CYP1B1 degrader-2. Its inhibitory properties make it suitable for studies related to drug metabolism and potential therapeutic applications.

Cat. No.

A69756

CAS No.

328087-38-3

Phortress

Synonyms: NSC 710305

Phortress is a potent cytochrome P450 inducer that specifically activates the aryl hydrocarbon receptor (AhR). By eliciting the transcription of CYP1A1, it demonstrates robust antitumor activity. This compound is valuable for research applications focused on drug metabolism, environmental toxicology, and the modulation of xenobiotic responses.

Cat. No.

A69759

CAS No.

615-16-7

2-Hydroxybenzimidazole

2-Hydroxybenzimidazole is a structural analog targeting CYP1A1, primarily utilized as a control ligand in structure-activity relationship studies of benzimidazole derivatives. This compound is inactive in terms of CYP1A1 induction, distinguishing it from other derivatives with thiol or amino substitutions. Its purpose is to serve as a baseline reference to better understand the biological activities of more active compounds in research applications.

Cat. No.

A69761

CAS No.

13164-03-9

Chalepensin

Chalepensin is a furanocoumarin that acts as a competitive inhibitor of the cytochrome P450 enzyme CYP2A6. In addition to its primary inhibitory effects on CYP2A6, Chalepensin has been shown to inhibit several other CYP enzymes, including CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4, albeit to varying degrees. This compound is valuable for research into drug metabolism and enzyme regulation, as well as for studies on the pharmacokinetics of therapeutic agents that undergo cytochrome P450-mediated biotransformation.

Cat. No.

A69762

CAS No.

189057-68-9

ZINC05626394

ZINC05626394 is a selective inhibitor of cytochrome b5 reductase 3, which enhances nitric oxide bioavailability. This compound demonstrates potential anti-cancer properties, particularly when used in conjunction with antibody-drug conjugates (ADCs) and immune checkpoint inhibitors. Its efficacy may be influenced by various resistance mechanisms, such as antigen-related resistance and endocytosis limitations, making it an intriguing candidate for further investigation in cancer research.

Cat. No.

A69764

CAS No.

2411389-67-6

PROTAC CYP1B1 degrader-1

PROTAC CYP1B1 Degrader-1 is a targeted degrader designed to selectively eliminate cytochrome P450 1B1 (CYP1B1), utilizing a α-naphthoflavone chimera derivative. This compound exhibits IC50 values of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2, demonstrating its specificity in degrading CYP1B1. It serves as a valuable tool for investigating the role of CYP1B1 in prostate cancer and may aid in overcoming CYP1B1-mediated drug resistance in therapeutic applications.

Cat. No.

A69765

CAS No.

582-16-1

2,7-Dimethylnaphthalene

2,7-Dimethylnaphthalene is a selective inhibitor of the cytochrome P450 1A2 (CYP1A2) enzyme, exhibiting an IC50 of 65 μM. This compound is important for investigating metabolic diseases and understanding the role of CYP1A2 in drug metabolism and toxicity. Its application in research can provide insights into enzyme regulation and the pharmacokinetics of various substrates.

Cat. No.

A69767

CAS No.

502654-40-2

CYP4A11/CYP4F2-IN-1

CYP4A11/CYP4F2-IN-1 is a potent dual inhibitor of cytochrome P450 enzymes CYP4A11 and CYP4F2, exhibiting IC50 values of 19 nM and 17 nM, respectively. This compound is valuable for studying the role of these enzymes in renal diseases and can aid in the development of targeted therapies. Its high specificity and effectiveness make it a crucial tool for researchers investigating cytochrome P450-mediated pathways.

Cat. No.

A69769

CAS No.

6515-36-2

7-Hydroxyflavanone

7-Hydroxyflavanone is a potent inhibitor of aromatase (CYP19), displaying an IC50 of 65 μM. This compound is known for its diverse biological activities, including anticarcinogenic and antioxidant properties, as well as exerting both estrogenic and anti-estrogenic effects. It is valuable for research applications focused on cancer biology, hormone regulation, and oxidative stress.