Cytochrome P450

Cat. No.

A69951

CAS No.

20697-20-5

Methysticin

Synonyms: DL-Methysticin; (±)-Methystici

Methysticin is a kavalactone derived from kava extract, primarily acting as an inducer of CYP1A1. This compound is relevant in studies investigating metabolic enzyme modulation and its impact on drug metabolism. Additionally, it has potential implications in understanding the biochemical pathways associated with liver function and detoxification processes.

Cat. No.

A69952

CAS No.

1370001-71-0

BMS-351

BMS-351 is a potent, orally active nonsteroidal inhibitor of CYP17A1 lyase, demonstrating IC50 values of 19 nM for human CYP17A1 and 4 nM for cynomolgus monkey CYP17A1. This compound is primarily utilized in research focused on castration-resistant prostate cancer, providing insights into hormonal regulation and potential therapeutic interventions in this challenging malignancy.

Cat. No.

A69956

CAS No.

1031063-36-1

(E/Z)-DMU2105

(E/Z)-DMU2105 is a selective inhibitor of CYP1B1, demonstrating potent inhibition with an IC50 value of 10 nM in yeast-derived microsomes and 63.65 nM in live recombinant yeast and human HEK293 kidney cells. This compound is valuable for research focused on cancer, glaucoma, ischemia, and obesity, offering insights into the role of CYP1B1 in various biological processes. Its specificity and potency make it a suitable tool for elucidating the function of this key enzyme in disease contexts.

Cat. No.

A69957

CAS No.

2241573-22-6

CYP11B2-IN-2

CYP11B2-IN-2 is a potent inhibitor of the aldosterone synthase enzyme CYP11B2, exhibiting an IC50 value of 0.3 nM. This compound is labeled with 18F, enabling its application as a positron emission tomography (PET) tracer for the diagnosis of primary aldosteronism. Its high specificity and efficacy make it a valuable tool for research in endocrine disorders and adrenal function.

Cat. No.

A69958

CAS No.

83219-99-2

10-Hydroxywarfarin

10-Hydroxywarfarin is a potent inhibitor of CYP2C9 and vitamin K epoxide reductase complex 1 (VKOR), exhibiting IC50 values of 1.6 µM and 80 ng/mL, respectively. This compound serves as a valuable tool in pharmacological research, particularly in studies related to anticoagulation therapies and vitamin K metabolism. Its role in influencing coagulation pathways makes it relevant for investigations into therapeutic strategies for thrombosis and related disorders.

Cat. No.

A69967

CAS No.

104890-70-2

(E/Z)-DMU2139

(E/Z)-DMU2139 is a potent and selective inhibitor of CYP1B1, exhibiting an IC50 value of 4 nM. This compound serves as a valuable tool for investigating the role of CYP1B1 in various biological processes and disease models. Its specificity and efficacy make it suitable for research aimed at understanding the mechanisms underlying CYP1B1-related pathways and the development of targeted therapies.

Cat. No.

A69981

CAS No.

4052-13-5

Cloperidone

Cloperidone is an inhibitor of cytochrome P450 2C9 (CYP2C9), demonstrating an IC50 of 17.7 μM. This compound has shown cytotoxic effects in HepG2 cells expressing CYP2C9, with a survival rate of 60% at a concentration of 10 μM. Cloperidone is valuable for studies investigating CYP2C9-related metabolic pathways and the effects of its inhibition in cellular models.

Cat. No.

A69987

CAS No.

25445-77-6

4-Phenyl-1,2,3-thiadiazole

4-Phenyl-1,2,3-thiadiazole is an inhibitor of cytochrome P450 enzymes CYP2B4 and CYP2E1. This compound effectively obstructs the oxidation of 1-phenylethanol to acetophenone, making it valuable for studies related to drug metabolism and enzymatic activity. Its ability to selectively inhibit these enzymes positions it as a significant tool for research in pharmacology and toxicology.

Cat. No.

A69988

CAS No.

2428734-45-4

CYP4Z1-IN-2

CYP4Z1-IN-2 is a reversible inhibitor of the enzyme CYP4Z1, displaying a Ki value of 2.2 μM. This compound effectively reduces the production of 14,15-EET in breast cancer cells and demonstrates an IC50 of 5.9 μM in inhibiting the CYP4Z1-mediated Luc-BE O-debenzylation reaction. CYP4Z1-IN-2 serves as a valuable tool for research focused on the role of CYP4Z1 in cancer biology and associated signaling pathways.

Cat. No.

A69993

CAS No.

2244569-14-8

DLCI-1

DLCI-1 is a selective oral inhibitor of cytochrome P450 2A6 (CYP2A6), demonstrating potent activity in modulating nicotine metabolism. This compound has been shown to significantly reduce nicotine self-administration in both male and female murine models, making it a valuable tool for research into nicotine addiction and metabolism. Its specificity towards CYP2A6 supports investigations into the therapeutic implications of targeting this enzyme in drug development and addiction studies.

Cat. No.

A69994

CAS No.

99957-90-1

Org30958

Org30958 is a potent inhibitor of cytochrome P450 enzymes, specifically targeting aromatase. This compound demonstrates significant biological activity in vivo, making it a valuable tool for researchers studying estrogen biosynthesis and related pathways. Its application extends to investigations of hormone-dependent cancers and metabolic disorders linked to altered P450 activity.

Cat. No.

A71399

CAS No.

675-20-7

2-Piperidone

Synonyms: δ-Valerolactam

2-Piperidone is an endogenous metabolite that serves as a biomarker for the activity of the cytochrome P450 enzyme CYP2E1. This compound is utilized in research applications aimed at understanding drug metabolism, toxicology, and the biochemical pathways involving liver function. Its relevance in pharmacokinetic studies makes it an important reagent for investigating the metabolic effects of various compounds.

Cat. No.

A76652

CAS No.

1315449-72-9

Osilodrostat phosphate

Synonyms: LCI699 phosphate

Osilodrostat phosphate is a selective inhibitor of 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2), demonstrating an IC50 of 35 nM and 0.7 nM, respectively, for human enzymes. This compound effectively inhibits the synthesis of aldosterone and corticosterone, contributing to its role in blood pressure regulation. Osilodrostat phosphate is particularly valuable for research investigating Cushing syndrome and related disorders involving dysregulated steroidogenesis.

Cat. No.

A78549

CAS No.

86831-54-1

Rhodiosin

Rhodiosin is a dual inhibitor of CYP2D6 and acetylcholinesterase (AChE), extracted from the root of Rhodiola rosea. It exhibits an IC50 value of 0.761 μM for CYP2D6 and a Ki of 0.769 μM. This compound demonstrates notable antioxidant and neuroprotective properties, contributing to the regulation of the HIF-1α signaling pathway, which is vital for central nervous system protection. Rhodiosin serves as a valuable tool for research in neuropharmacology and metabolic studies.

Cat. No.

A84993

CAS No.

2952994-34-0

YXG-158

YXG-158 is an orally active androgen receptor (AR) degrader and CYP17A1 inhibitor. It exhibits AR degradation activity with a DC50 value of 1.28 μM and inhibits CYP17A1 with an IC50 value of 100 nM. This compound is particularly relevant for research applications focused on enzalutamide-resistant prostate cancer, providing a valuable tool for investigating therapeutic strategies in this context.

Cat. No.

A87943

CAS No.

3189-22-8

7-Methoxyindole, 98%

7-Methoxyindole is a potent interactor of cytochrome P450 enzymes. This compound is utilized in research focused on drug metabolism and toxicity, as it plays a critical role in the modulation of enzymatic activity. Its pharmacological properties make it suitable for studies investigating the metabolic pathways of various xenobiotics and endogenous compounds.

Cat. No.

B15125

CAS No.

66841-24-5

(1R,2S,1'R)-Cypermethrin

(1R,2S,1'R)-Cypermethrin is a specific isomer of the pyrethroid pesticide Cypermethrin, classified as Class II due to its moderate toxicity. This compound exhibits significant neurotoxic activity by interacting with voltage-gated sodium channels, leading to prolonged neuronal depolarization. (1R,2S,1'R)-Cypermethrin is primarily employed in research focusing on its effects on nervous system function and insecticidal action. Its ability to cross the blood-brain barrier allows for studies on its impact on both invertebrate and vertebrate models.

Cat. No.

B21899

CAS No.

69097-98-9

(±)Homoeriodictyol (racemic)

(±) Homoeriodictyol is a potent inhibitor of aromatase (CYP19), an enzyme critical in estrogen biosynthesis. This compound is primarily utilized in breast cancer research to investigate estrogen-mediated pathways and their role in tumor growth. Its inhibitory activity makes it a valuable tool for studying therapeutic strategies targeting aromatase in hormone-related cancers.