Cytochrome P450

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.

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.

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.

Cat. No.

A69770

CAS No.

52601-58-8

CYP1B1-IN-7

CYP1B1-IN-7 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1, exhibiting an IC50 value of 75 nM. This compound effectively reverses drug resistance in cancer cells, demonstrating an IC50 of 29 µM in the CYP1B1-overexpressing MCF-7 cell line resistant to Docetaxel. Its ability to induce cytotoxicity in resistant cell lines makes it a valuable tool for research on pharmacoresistance and the development of targeted cancer therapies.

Cat. No.

A69775

CAS No.

19993-32-9

Thermopsoside

Thermopsoside is a flavone derivative that functions as a specific inhibitor of CYP3A4. Demonstrating inhibitory effects on various CYP450 isozymes, it exhibits IC50 values of 6.0 μM for CYP3A4, alongside inhibitory activities against CYP2C19, CYP2D6, and CYP2C9 at concentrations of 9.5 μM, 12.0 μM, and 32.0 μM, respectively. This compound is valuable for research focused on drug metabolism and pharmacokinetics, particularly in studies exploring drug interactions mediated by CYP450 enzymes.

Cat. No.

A69777

CAS No.

786-97-0

SU 10603

SU 10603 is a specific inhibitor of cytochrome P45017A1 (CYP17A1). It effectively blocks the enzymatic activity responsible for the conversion of pregnenolone and progesterone into androgens, thereby regulating steroidogenesis. This compound is utilized in research applications related to hormone-driven conditions such as prostate cancer and adrenal hyperplasia, facilitating studies on the modulation of androgen levels.

Cat. No.

A69778

CAS No.

1174416-41-1

Dasatinib analog-1

Dasatinib analog-1 is a potent inhibitor of CYP3A4, achieving a Ki value of 5.4 μM. This compound effectively blocks the formation of glutathione adducts, making it valuable for studying drug metabolism and interactions. Its ability to modulate CYP3A4 activity positions it as a useful tool in pharmacological research and toxicology studies.

Cat. No.

A69780

CAS No.

62218-08-0

ε-Viniferin (epsilon-Viniferin)

Synonyms: epsilon-Viniferin

ε-Viniferin, a dimer of resveratrol, serves as a potent inhibitor of cytochrome P450 enzymes, exhibiting Ki values ranging from 0.5 to 20 μM. This compound is shown to possess significant antioxidant, anti-inflammatory, anti-diabetic, and anti-neurodegenerative properties. Its diverse biological activities make ε-Viniferin a valuable tool for research in pharmacology, toxicology, and disease models related to oxidative stress and inflammation.

Cat. No.

A69783

CAS No.

21535-97-7

3-Methylbenzofuran

3-Methylbenzofuran is a specific inhibitor of the cytochrome P450 enzyme CYP2A6, exhibiting an IC50 of 7.35 μM. This compound is particularly relevant for studies investigating tobacco-related carcinogenesis, providing insights into metabolic pathways involved in the activation of tobacco-derived carcinogens. Its role in modulating CYP2A6 activity makes it a valuable tool in chemical research focused on cancer biology and pharmacology.

Cat. No.

A69789

CAS No.

1356479-78-1

CYP11B2-IN-1

CYP11B2-IN-1 is a potent inhibitor of CYP11B2, exhibiting an IC50 of 2.3 nM. Additionally, it demonstrates inhibitory activity against CYP11B1 with an IC50 of 142 nM. This compound is primarily utilized in research focused on steroidogenesis, hypertension, and cardiovascular diseases. Its selective inhibition properties make it a valuable tool for studying adrenal enzymatic pathways and developing therapeutic strategies.

Cat. No.

A69790

CAS No.

1314116-53-4

Clopidogrel-β-D-glucuronide

Clopidogrel-β-D-glucuronide is an inhibitor of the CYP2C8 enzyme. As a metabolite of Clopidogrel, it selectively binds to CYP2C8, resulting in significant inhibition of this liver enzyme's activity. This compound plays a crucial role in understanding drug metabolism and interactions, making it valuable for research applications in pharmacology and toxicology.

Cat. No.

A69791

CAS No.

841-73-6

Bucolome

Synonyms: Paramidin; Paramidine

Bucolome is a selective inhibitor of cytochrome P450 2C9 (CYP2C9), primarily used for its uricosuric and anti-inflammatory properties. Its mechanism of action facilitates the increased excretion of uric acid, making it valuable in the research of hyperuricemia and related conditions. Bucolome's modulation of CYP2C9 activity also provides a useful tool for studying drug metabolism and interactions in pharmacological research.

Cat. No.

A69792

CAS No.

94356-22-6

Rhapontigenin 3'-O-glucoside

Rhapontigenin 3'-O-glucoside is a derivative of Rhapontigenin, functioning primarily as an inhibitor of cytochrome P450 enzymes, particularly human P450 1A1. This compound exhibits notable biological activity in modulating enzymatic pathways associated with drug metabolism and carcinogenesis. Its potential applications in cancer chemoprevention research make it a valuable reagent for studies examining the role of P450 enzymes in oncogenic processes.

Cat. No.

A69794

CAS No.

193079-69-5

Tabimorelin

Synonyms: NN703

Tabimorelin is a potent inhibitor of the CYP3A4 enzyme. This compound is recognized for its ability to act as an orally active growth hormone (GH) secretagogue, stimulating the release of GH in a physiological context. Its dual role as a CYP3A4 inhibitor has implications in drug metabolism studies and in understanding pharmacokinetic interactions. Tabimorelin is utilized in research related to endocrine function and therapeutic applications in conditions characterized by GH deficiency.

Cat. No.

A69798

CAS No.

502656-68-0

CAY 10462 dihydrochloride

CAY 10462 dihydrochloride is a potent inhibitor of CYP4A hydroxylase. This compound enhances the contractile response to angiotensin II, demonstrating a maximal contractile response (Emax) at 6764 mg. CAY 10462 dihydrochloride is valuable for research focused on cardiovascular physiology and metabolic pathways involving cytochrome P450 enzymes.

Cat. No.

A69800

CAS No.

18110-87-7

4,5-Dimethoxycanthin-6-one

4,5-Dimethoxycanthin-6-one is a potent uncompetitive inhibitor of CYP1A2, exhibiting an IC50 value of 1.7 μM and a Ki value of 2.6 μM in phenacetin O-deethylation assays. This alkaloid, derived from the wood of Picrasma quassioides BENNET (Simaroubaceae), serves as a valuable tool for studying CYP1A2-mediated drug metabolism and interactions. Its inhibitory properties make it suitable for research applications in pharmacology and toxicology.

Cat. No.

A69803

CAS No.

112560-33-5

Keto-itraconazole

Synonyms: keto-ITZ

Keto-itraconazole, a potent inhibitor of CYP3A, is a metabolite of Itraconazole. It demonstrates a significant unbound IC50 value of 4.6 nM when assessed using human liver microsomes in conjunction with midazolam. This compound is valuable for research focused on drug metabolism and interactions involving CYP3A-mediated pathways.

Cat. No.

A69804

CAS No.

4430-31-3

Octahydrocoumarin

Octahydrocoumarin is a potent inhibitor of the cytochrome P450 enzyme CYP2A13, exhibiting an IC50 value of 6.6 μM. This compound's inhibition of CYP2A13 makes it a valuable tool for investigating drug metabolism and potential interactions in chemical research. It is particularly relevant for studies related to the metabolism of various xenobiotics and therapeutic agents.

Cat. No.

A69809

CAS No.

912291-11-3

CYP2A6-IN-2

CYP2A6-IN-2 is a selective inhibitor of the cytochrome P450 isoform CYP2A6. This compound is primarily utilized in research focused on elucidating the mechanisms underlying nicotine dependence and metabolism. Its inhibition of CYP2A6 may provide valuable insights into the pharmacological profiles of nicotine and other substrates metabolized by this enzyme, facilitating the development of therapeutic strategies for addiction and related disorders.

Cat. No.

A69810

CAS No.

2305-05-7

γ-Dodecanolactone

γ-Dodecanolactone acts as an inhibitor of the cytochrome P450 enzyme CYP1A2, demonstrating an IC50 value of 58 µM and a pIC50 value of 4.24. This γ-lactone compound is suitable for studies investigating the biological implications of CYP1A2 inhibition, particularly in the context of diseases associated with this enzyme. Researchers can utilize γ-Dodecanolactone to explore metabolic pathways and drug interactions involving CYP1A2.

Cat. No.

A69812

CAS No.

1375603-36-3

Seviteronel racemate

Synonyms: VT-464 (racemate)

Seviteronel racemate is a potent inhibitor of cytochrome P450 17A1 (CYP17), specifically targeting the lyase activity associated with this enzyme. With a low nanomolar IC50 value, it effectively disrupts steroidogenesis, making it valuable for research into conditions related to hormone regulation and hormonal therapies. This compound is suitable for studies focused on cancer biology, particularly in understanding the mechanisms underlying testosterone biosynthesis in prostate cancer.