Cytochrome P450

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.

Cat. No.

A69895

CAS No.

82475-00-1

5,7,2',6'-Tetrahydroxyflavone

5,7,2',6'-Tetrahydroxyflavone is a natural flavonoid that functions as a selective inhibitor of CYP3A4, impacting the hepatic metabolism of steroids. It demonstrates significant biological activity with an IC50 value of 7.8 μM, making it a valuable tool for research on testosterone metabolism and drug interactions. This compound is particularly useful for studies investigating the modulation of cytochrome P450 enzymes in pharmacological and toxicological contexts.

Cat. No.

A69897

CAS No.

3053864-59-5

CYP51-IN-21

CYP51-IN-21 is a potent inhibitor of cytochrome P450 51 (CYP51), demonstrating significant antifungal activity against various pathogenic fungi, including drug-resistant strains. By targeting CYP51, CYP51-IN-21 disrupts the biosynthesis of essential sterols, impairing fungal growth and viability. Additionally, CYP51-IN-21 effectively inhibits the formation of fungal biofilms, making it a valuable candidate for research in antifungal therapeutics and biofilm-related studies.

Cat. No.

A69900

CAS No.

72963-72-5

Imiprothrin

Imiprothrin is a potent inducer of CYP1A2, known for its significant effects on metallothionein 1a expression. This compound exhibits genotoxic and cytotoxic properties, evident through the initiation of detoxification responses in rat hepatocytes and the induction of chromosomal aberrations and micronucleus formation in bone marrow cells. Additionally, Imiprothrin prompts oxidative stress, resulting in lipid peroxidation and reactive oxygen species production, which can adversely affect liver and kidney functions. Though it inhibits weight gain and can lead to high mortality in female mice at elevated doses, it has not shown carcinogenicity in rat studies, with sensitive toxicity biomarkers including aspartate aminotransferase and total protein.

Cat. No.

A69904

CAS No.

24563-03-9

Dihydrocubebin

Synonyms: (-)-Dihydrocubebin

Dihydrocubebin is a selective inhibitor of cytochrome P450 3A4 (CYP3A4), a key enzyme involved in drug metabolism. Isolated from Piper cubeba, it demonstrates potent inhibitory effects, making it a valuable tool for studying CYP3A4-related metabolic processes. Its role in research applications includes evaluating drug interactions and understanding the metabolic pathways of pharmaceutical compounds.

Cat. No.

A69910

CAS No.

75412-96-3

2-Methoxy-5-acetoxyfuranogermacr-1(10)-en-6-one

2-Methoxy-5-acetoxyfuranogermacr-1(10)-en-6-one is a potent aromatase (CYP19) inhibitor, exhibiting an IC50 value of 0.21 μM against human targets. This compound is particularly relevant for research in breast cancer, providing insights into estrogen synthesis regulation and its implications in cancer progression. Its use in preclinical studies may advance the understanding of therapeutic strategies targeting estrogen-dependent tumors.

Cat. No.

A69913

CAS No.

183012-13-7

YM116

YM116 is a potent and orally active competitive inhibitor of CYP17A1, with a reported Ki of 0.38 nM. By specifically inhibiting the C17-20 lyase activity, YM116 effectively reduces the synthesis of adrenal androgens, leading to decreased serum testosterone levels and lower dehydroepiandrosterone sulfate concentrations. This compound is valuable for research applications involving androgen-related disorders and prostate health.

Cat. No.

A69916

CAS No.

3077254-39-5

CYP1B1-IN-9

CYP1B1-IN-9 is a highly selective competitive inhibitor of CYP1B1, demonstrating an IC50 of 1.48 nM. It effectively inhibits the migration and invasion of A549/T cells and has been shown to resensitize cells resistant to Paclitaxel. Notable for its favorable pharmacokinetic properties, metabolic stability, and safety profile, CYP1B1-IN-9 serves as a valuable tool for investigating tumor-drug resistance mechanisms in cancer research.

Cat. No.

A69917

CAS No.

1370702-83-2

7ETMC

7ETMC is a selective inhibitor of human cytochrome P450 enzymes 1A1 and 1A2. It exhibits potent inhibitory activity, with IC50 values of 0.46 μM and 0.50 μM, respectively, demonstrated within the first six minutes of exposure. Notably, 7ETMC does not inhibit cytochrome P450 enzymes 2A6 and 2B1. This compound may be valuable for research applications involving drug metabolism and the study of enzyme activity related to these particular cytochrome P450 isoenzymes.

Cat. No.

A69919

CAS No.

67667-71-4

8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate

8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate functions as an irreversible inhibitor of CYP2A6, exhibiting IC50 values of 8.64 μM and 22.3 μM under pre-incubation and co-incubation conditions, respectively. Additionally, this compound demonstrates inhibitory activity against monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B), with IC50 values of 60.2 μM and 38.6 μM, respectively. It serves as a valuable tool for research involving drug metabolism, neurochemistry, and the study of pharmacological responses influenced by these metabolic pathways.

Cat. No.

A69922

CAS No.

1373353-95-7

GW694481

GW694481 is a selective inhibitor of CYP2C9 and CYP3A4, exhibiting IC50 values of 2.1 μM and 17.0 μM, respectively. This compound functions as an ApoA1 upregulator, enhancing the expression of ApoA1 in human hepatic cells. GW694481 is valuable for research focused on atherosclerosis and related metabolic disorders, providing insights into lipid metabolism and cardiovascular health.

Cat. No.

A69929

CAS No.

790676-41-4

(R)-N-3-Benzylnirvanol

(R)-N-3-Benzylnirvanol is the R-isomer of the racemic compound (±)-N-3-Benzylnirvanol, consisting of both (+)-N-3-Benzylnirvanol and (-)-N-3-Benzylnirvanol. This compound serves as a potent and selective inhibitor of cytochrome P450 enzymes, specifically exhibiting a Ki value of 0.25 μM for CYP2C19. Research applications include the study of drug metabolism and interactions, as well as pharmacological investigations targeting cytochrome P450-mediated pathways.

Cat. No.

A69932

CAS No.

2836297-26-6

PROTAC CYP1B1 degrader-2

PROTAC CYP1B1 degrader-2 is a VHL E3 ligase-based degrader targeting CYP1B1, exhibiting a DC50 of 1.0 nM in A549/Taxol cells after 24 hours. This compound effectively inhibits the growth, migration, and invasion of cancer cells, making it a valuable tool for research into the therapeutic potential of targeting CYP1B1 in cancer treatment. Its unique mechanism of action offers insights into the modulation of protein levels in various biological contexts.

Cat. No.

A69933

CAS No.

3003751-14-9

hCYP3A4-IN-1

hCYP3A4-IN-1 is a potent inhibitor of human cytochrome P450 3A4 (hCYP3A4) with notable activity in both human liver microsomes and CHO-3A4 stable cell lines, exhibiting IC50 values of 43.93 nM and 153.00 nM, respectively. This inhibitor effectively blocks CYP3A4-mediated hydroxylation of N-ethyl-1,8-naphthalimide (NEN) in a competitive manner, with a Ki of 30.00 nM. hCYP3A4-IN-1 is valuable for research applications focused on drug metabolism and interactions involving CYP3A4.

Cat. No.

A69935

CAS No.

242143-80-2

Tabimorelin hemifumarate

Synonyms: NN703 hemifumarate

Tabimorelin hemifumarate is a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound functions as a growth hormone secretagogue, promoting the secretion of growth hormone in the body. Its key biological activities make it valuable for research applications in endocrine signaling and pharmacokinetics, particularly in studies assessing drug metabolism and interactions involving CYP3A4.

Cat. No.

A69940

CAS No.

769917-29-5

CAY 10434

CAY 10434 is a potent inhibitor of CYP4A hydroxylase, demonstrating significant effects on vascular smooth muscle contractility. This compound enhances the contractile response to angiotensin II, achieving a maximal contractile response (Emax) of 6764 mg. CAY 10434 is valuable for research into cardiovascular physiology and the regulatory mechanisms underlying vascular reactivity.

Cat. No.

A69943

CAS No.

3072732-90-9

CYP11B2-IN-3

CYP11B2-IN-3 is a selective inhibitor of CYP11B2, demonstrating an IC50 value of 12.92 nM for CYP11B2 and 2341 nM for CYP11B1. This compound is orally active, making it suitable for in vivo studies. CYP11B2-IN-3 is primarily applicable in research related to hypertension, providing a valuable tool for investigating the role of CYP11B2 in adrenal steroidogenesis and blood pressure regulation.

Cat. No.

A69944

CAS No.

46992-81-8

Peucedanol

Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM, while functioning as a competitive inhibitor of CYP1A2 and CYP2D6, with Ki values of 3.39 μM and 6.77 μM, respectively. This compound plays a significant role in pharmacological research by modulating drug metabolism pathways. Its ability to inhibit key cytochrome P450 enzymes makes it a valuable tool for studies examining drug interactions and metabolic regulation.

Cat. No.

A69945

CAS No.

92981-78-7

Tesmilifene hydrochloride

Tesmilifene hydrochloride is a cytochrome P450 inhibitor with notable implications in cancer research. This compound displays hormonal activity that affects DNA synthesis in MCF-7 cells and has been shown to stimulate tumor growth in mouse and rat models. Tesmilifene hydrochloride is particularly relevant for studies investigating the mechanisms of multidrug resistance in cancer therapeutics.

Cat. No.

A69946

CAS No.

288323-41-1

Thienyldecyl Isothiocyanate

Thienyldecyl Isothiocyanate serves as a cytochrome P450 modulator, demonstrating significant antiproliferative activity against cancer cells. This compound exerts its effects through the inhibition of cytochrome P450 enzymes and the induction of phase II detoxification enzymes, impacting xenobiotic metabolism. Thienyldecyl isothiocyanate is valuable for research in cancer biology and pharmacology, particularly in studies exploring enzyme modulation and its implications for drug metabolism and efficacy.

Cat. No.

A69948

CAS No.

117038-80-9

Licopyranocoumarin

Licopyranocoumarin is an isoflavonoid known for its inhibitory action on the cytochrome P450 enzyme CYP3A4, exhibiting an IC50 of 32 μM. This compound also demonstrates significant neuroprotective properties, making it a valuable reagent for studies focused on drug metabolism and neurodegenerative disorders. Researchers may utilize Licopyranocoumarin to explore its effects on enzyme activity and potential therapeutic applications in neurological research.

Cat. No.

A69949

CAS No.

842122-33-2

CYP1B1-IN-1

CYP1B1-IN-1 is a selective inhibitor of cytochrome P450 1B1 (CYP1B1) with an IC50 value of 0.49 nM. This compound is valuable for studying the role of CYP1B1 in various biological processes, including the metabolism of xenobiotics and the activation of pro-carcinogens. CYP1B1-IN-1 is suitable for research applications focused on cancer biology and toxicology, providing insights into the pharmacological modulation of CYP1B1 activity.

Cat. No.

A69950

CAS No.

73804-65-6

11-HETE

Synonyms: 11-Hydroxy-5,8,12,14-eicosatetraenoic acid

11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) serves as an activator for cytochrome P450 enzymes. This compound is known to upregulate the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, leading to significant biological effects such as cell hypertrophy in RL-14 cells. Due to its modulatory role in cytochrome P450 activity, 11-HETE holds potential applications in the study of cardiovascular diseases.