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Ketoconazole

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Ketoconazole is a laboratory reagent commonly used as an antifungal agent. It functions as an inhibitor of the cytochrome P450 enzyme system, specifically targeting the CYP3A4 isoform. Ketoconazole is often utilized in various research applications that require the modulation of CYP3A4 activity.

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Lab products found in correlation

Cobicistat, by MedChemExpress (3 mentions) Peg400, by Merck Group (3 mentions) Ch223191, by MedChemExpress (2 mentions) Corn oil, by Merck Group (2 mentions) Anti btk, by Cell Signaling Technology (2 mentions) Polysorbate 80 tween 80, by Merck Group (2 mentions) Fvb wild type mice, by Taconic Biosciences (2 mentions) Peg300, by Merck Group (2 mentions) Acetonitrile, by Thermo Fisher Scientific (2 mentions) Lc ms grade formic acid, by Thermo Fisher Scientific (1 mentions) Ibrutinib, by Alsachim (1 mentions) Deoxycholic acid, by Merck Group (1 mentions) Z guggulsterone, by Santa Cruz Biotechnology (1 mentions) Jte 013, by Merck Group (1 mentions) Kg 501, by MedChemExpress (1 mentions) Methoctramine, by Adooq (1 mentions) Srebp2 antibody, by R&D Systems (1 mentions) Fatostatin, by MedChemExpress (1 mentions) Lovastatin, by MedChemExpress (1 mentions) Ketoconazole, by Merck Group (1 mentions)

9 protocols using ketoconazole

1

Exploring LPS-induced Cell Viability and Gene Expression in hPDLCs

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Cell activity was measured by a CCK-8 assay (KitkGA317S-500, KeyGEN BioTECH, China). hPDLCs were cultured in 96-well plates and treated with Pg-LPS (InvivoGen, San Diego, USA) at different concentrations (0, 0.1, 1, 5, 10, and 20 µg/ml) for 24 hours. CCK-8 solution was added to each well for 10 µL and incubated at 37℃ for 3 hours for the cell viability assay. Cell viability was determined by reading absorbance at 450 nm using a microplate reader.
Cell stimulation hPDLCs were seeded in 6-well plates and divided into the following two groups-the control group and Pg-LPS treatment group (LPS) to observe the key genes expressions. Besides, in order to explore whether KIAA0125 and CYP24A1 have a co-expression relationship in an in ammatory environment, hPDLCs were divided into four groups: Pg-LPS treatment group (LPS), 1,25-dihydroxyvitamin D3 (1,25D) (Sigma Aldrich, Saint Louis, MO, USA) and Pg-LPS treatment group (1,25D + LPS), 1,25D and Pg-LPS plus low concentrations of ketoconazole (MedChem Express, Monmouth Junction, USA) group (1,25D + LPS + 10 µM ketoconazole), and 1,25D and Pg-LPS plus high concentrations of ketoconazole group (1,25D + LPS + 100 µM ketoconazole). The concentration of Pg-LPS was 1 µg/mL and 1,25D was 10 nM. The incubation period was 24 hours.
Li Y., Li R., Wu Y., Gong C., & Ding X. (2020). Identification the Synergistic Effect of Immune-Related lncRNA KIAA0125 and Vitamin D Metabolism Related Gene CYP24A1 in Periodontitis.
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2

Regulation of Cellular Signaling Pathways

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All chemicals, including IS and ketoconazole, were from Sigma-Aldrich (St. Louis, MI, USA) unless otherwise stated. IS was used at concentrations of 2 μM and 4 μM, which correspond to the normal human serum concentration of IS [53 (link),95 (link),96 (link)]. The aryl hydrocarbon receptor (AHR) inhibitor, CH223191, was obtained from MedChemExpress (MCE, Monmouth Junction, NJ, USA) and was applied at a concentration of 10 μM. Pregnane X receptor (PXR) downstream signaling was inhibited using ketoconazole at a final concentration of 25 μM [75 (link),76 (link)].
Sári Z., Mikó E., Kovács T., Boratkó A., Ujlaki G., Jankó L., Kiss B., Uray K, & Bai P. (2020). Indoxylsulfate, a Metabolite of the Microbiome, Has Cytostatic Effects in Breast Cancer via Activation of AHR and PXR Receptors and Induction of Oxidative Stress. Cancers, 12(10), 2915.
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3

Quantitative Analysis of Ibrutinib

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Ibrutinib was purchased from LC Labs. Cobicistat and ketoconazole were purchased from MedChemExpress. Reference standards of Ibrutinib, its primary metabolite PCI-45227 (M37) and their corresponding deuterated versions, used as internal standards for the analytic method, were purchased from AlsaChim. PEG300, PEG400, corn oil, and polysorbate-80 (Tween-80) were purchased from Sigma-Aldrich, and LC-MS–grade formic acid (FA), methanol, and acetonitrile were from Thermo Fisher Scientific. Blank plasma was obtained from FVB wild-type mice (Taconic Biosciences). The following antibodies were obtained from Cell Signaling Technology: anti-BTK (catalog no. 8547). Anti-phospho-BTK (Y223, catalog no. ab68217) was purchased from Abcam and anti-GAPDH (catalog no. MAB374) was purchased from Millipore Sigma.
Eisenmann E.D., Fu Q., Muhowski E.M., Jin Y., Uddin M.E., Garrison D.A., Weber R.H., Woyach J.A., Byrd J.C., Sparreboom A, & Baker S.D. (2021). Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition. Cancer Research Communications, 1(2), 79-89.
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4

Molecular Regulators of Lipid Metabolism

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Deoxycholic acid and JTE-013 were obtained from Sigma-Aldrich (St. Louis, MO, USA). Triamterene, 4-DAMP, ketoconazole, lovastatin, KG-501 and fatostatin were purchased from MedChemexpress (Monmouth Junction, NJ, USA). Methoctramine was from AdooQ Bioscience (Nanjing, China). Z-Guggulsterone was from Santa cruz Biotechnology (Santa cruz, CA, USA). SREBP2 antibody was obtained from R&D Systems (Minneapolis, MN, USA).
Li D., Zhou J., Wang L., Gong Z., Le H., Huang Y., Xu C., Tian C., Cai W, & Wu J. (2023). Gut microbial metabolite deoxycholic acid facilitates Th17 differentiation through modulating cholesterol biosynthesis and participates in high-fat diet-associated colonic inflammation. Cell & Bioscience, 13, 186.
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5

Investigating Aryl Hydrocarbon and Pregnane X Receptor Modulation

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Chemicals, among them, indolepropionic acid (IPA), glutathione (GSH), N-acetyl-cysteine (NAC), Mito-TEMPO, and ketoconazole were from Sigma-Aldrich (St. Louis, MO, USA) unless otherwise stated. IPA was used, 0.4 μM and 0.8 μM, which corresponds to the normal human serum concentration of IPA [40 (link),49 (link),50 (link)]. GSH and NAC antioxidants were used at a final concentration of 5 mM. The mitochondria-targeted antioxidant Mito-TEMPO was used at a concentration of 5 μM. The aryl hydrocarbon receptor (AHR) inhibitor, CH223191, was obtained from MedChemExpress (MCE, Monmouth Junction, NJ, USA) and was applied at a concentration of 10 μM. Pregnane X receptor (PXR) downstream signaling was inhibited using ketoconazole at a final concentration of 25 μM [51 (link),52 (link)]. The Silencer Select siRNAs targeting AHR (AHR—siRNA ID: s1198) and PXR (NR1I2—siRNA ID: s16910) and the negative control siRNA #1 (cat.no. 4390843) were obtained from Thermo Fisher Scientific (Waltham, MA, USA) and each was used at a final concentration of 30 nM.
Sári Z., Mikó E., Kovács T., Jankó L., Csonka T., Lente G., Sebő É., Tóth J., Tóth D., Árkosy P., Boratkó A., Ujlaki G., Török M., Kovács I., Szabó J., Kiss B., Méhes G., Goedert J.J, & Bai P. (2020). Indolepropionic Acid, a Metabolite of the Microbiome, Has Cytostatic Properties in Breast Cancer by Activating AHR and PXR Receptors and Inducing Oxidative Stress. Cancers, 12(9), 2411.
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6

GC20 Purity Analysis by LC-MS/MS

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GC20 (purity > 99%) was supplied by the Department of Pharmacology, Shanghai Institute of Pharmaceutical Industry (Shanghai, China). Ketoconazole (internal standard, IS) was purchased from MedChemExpress (Monmouth Junction, NJ, USA). Methanol, formic acid, and ammonium formate were analytical grade and purchased from Sigma-Aldrich (St. Louis, MO, USA). Ultrapure water was prepared by Milli-Q Ultrapure water purification system (Millipore, Bedford, MA, USA).
Peng Y., Qi H., Chang Q., Zhang Y., Liu W., Liu M., Liu Q., Wang G, & Sun J. (2019). Pharmacokinetics and Tissue Distribution of a Novel Bis-Chelated Gold(I) Diphosphine Compound, Bis(2,3-bis(tert-butylmethylphosphino)Quinoxaline)Aurate(I), in Rats. Molecules, 24(11), 2082.
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7

Multimodal Cancer Therapy Protocol

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Ketoconazole (Catalog no. K1003) was purchased from MedChemExpress, IR780 iodide (Catalog no. 207399‐07‐3), 3‐bromopropylamine hydrobromide, hyaluronidase (Catalog no.37326‐33‐3), and triphenylphosphine were obtained from J&K Scientific. 1,3‐Diphenylisobenzofuran (DPBF), dimethyl sulfoxide (DMSO), chondroitin sulfate (Catalog no. 24967‐93‐9), and crystal violet (Catalog no. C0775) were purchased from Aladdin Industrial Corporation. The One Step TUNEL Apoptosis Assay Kit was purchased from Beyotime Biotechnology. Mito‐Tracker Green and Hoechst 33342 were bought from Life Technologies. Penicillin and streptomycin were acquired from Millipore Sigma. RiboBio Co. supplied the EdU labeling test kit (C10310‐1). Mouse IL‐2 ELISA Kit (EK202/2‐01), and mouse TNF‐alpha ELISA Kit (GEM0004) was received from Elabscience. The types of antibodies used are as follows: PARP, caspase 3, and p62 were acquired from Cell Signaling Technology; LC3 was received from Novus. CRT Rabbit Monoclonal Antibody (WL04297), Ki67 (bsm‐33 070 M), and HMGB1 Rb pAb (WL03023) were obtained from WanLeibio.
Liu S., Tian H., Ming H., Zhang T., Gao Y., Liu R., Chen L., Yang C., Nice E.C., Huang C., Bao J., Gao W, & Shi Z. (2024). Mitochondrial‐Targeted CS@KET/P780 Nanoplatform for Site‐Specific Delivery and High‐Efficiency Cancer Immunotherapy in Hepatocellular Carcinoma. Advanced Science, 11(14), 2308027.
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8

In Vitro Evaluation of Venetoclax Interactions

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Venetoclax, rifampin, ritonavir, cobicistat, ketoconazole, fluconazole, itraconazole voriconazole, posaconazole, isavuconazole, micafungin, caspofungin, and anidulafungin were purchased from MedChemExpress (Monmouth Junction, NJ, USA). The major itraconazole metabolites, hydroxy-itraconazole and keto-itraconazole were kindly provided by Dr. Nina Isoherranen (University of Washington, Seattle, WA, USA). [3H]Estradiol-17β-D-glucuronide (EβG; specific activity, 50.1 Ci/mmol), a positive control substrate for OATP1B, was purchased from American Radiolabeled Chemicals (Saint Louis, MO, USA). [3H]Venetoclax (specific activity, 29.3 Ci/mmol) was obtained from ViTrax (Placentia, CA, USA). PEG400 was purchased from Sigma-Aldrich (Burlington, MA, USA). Dimethyl sulfoxide (DMSO), LC-MS-grade formic acid, methanol, and acetonitrile were purchased from Fisher Scientific (Fair Lawn, NJ, USA), and 8-acetoxy-trisulfopyrene was obtained from Carbosynth Limited (Compton, Berkshire, UK). Human recombinant CYP3A4 Supersomes (456207) was purchased from Corning (Glendale, AZ, USA). NADPH RapidStart Regenerating System was purchased from SEKISUI XenoTech (Kansas City, KS, USA).
Eisenmann E.D., Garrison D.A., Talebi Z., Jin Y., Silvaroli J.A., Kim J.G., Sparreboom A., Savona M.R., Mims A.S, & Baker S.D. (2022). Interaction of Antifungal Drugs with CYP3A- and OATP1B-Mediated Venetoclax Elimination. Pharmaceutics, 14(4), 694.
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9

Quantification of Ibrutinib and Metabolite in Plasma

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Ibrutinib was purchased from LC-Labs (Woburn, MA). Cobicistat and ketoconazole were purchased from MedChemExpress (Monmouth Junction, NJ). Reference standards of ibrutinib, its primary metabolite PCI-45227 (M37) and their corresponding deuterated versions, used as internal standards for the analytical method, were purchased from AlsaChim (Illkirch-Graffenstaden, France). PEG300, PEG400, corn oil, and polysorbate-80 (Tween-80) were purchased from Sigma-Aldrich (Burlington, MA), and LC-MS-grade formic acid (FA), methanol, and acetonitrile were from Fisher Scientific (Fair Lawn, NJ). Blank plasma was obtained from FVB wild-type mice (Taconic Biosciences, Cambridge City, IN). The following antibodies were obtained from Cell Signaling (Danvers, MA): anti-BTK (Cat. #8547). Anti-phospho-BTK (Y223, Cat. #ab68217) was purchased from Abcam (Cambridge, MA) and anti-GAPDH (Cat. #MAB374) was purchased from Millipore Sigma (Burlington, MA).
Eisenmann E.D., Fu Q., Muhowski E.M., Jin Y., Uddin M.E., Garrison D.A., Weber R.H., Woyach J.A., Byrd J.C., Sparreboom A, & Baker S.D. (2021). Intentional Modulation of Ibrutinib Pharmacokinetics through CYP3A Inhibition. Cancer Research Communications, 1(2), 79-89.
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