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CYP17 inhibitor
Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues.
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CYP17 inhibitor
Alizarin is novelly used as a staining agent in biological research because it stains free calcium and certain calcium compounds a red or light purple color.- Tianxing Ying, .et al. , Cancers (Basel), 2022, Dec 30;15(1):243 PMID: 36612238
- Ryota Kitakami, .et al. , Bioorg Med Chem, 2021, Jun 26;44:116292 PMID: 34225167
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Protein kinase inhibitor
Apigenin, found in many plants, is a natural product belonging to the flavone class that is the aglycone of several naturally-occurring glycosides. Apigenin acts as a monoamine transporter activator, one of the few chemicals demonstrated to possess this property. Apigenin is a ligand for central benzodiazepine receptors that competitively inhibited the binding of flunitrazepam with a Ki of 4μM, exerting anxiolytic and slight sedative effects.
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CYP17 inhibitor
Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) inhibitor.- Yuyan Zhu, .et al. , Metabolism, 2021, Oct;123:154861 PMID: 34371065
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Lipoxygenase Inhibitor
Baicalein is a flavonoid originally isolated from the roots of Scutellaria baicalensis Georgi. Baicalein inhibits lipid peroxidation, as assessed by production of TBARS, with an IC50 value of 5 µM.
- Wafa Naji Shnaikat, .et al. , Iraqi J Pharm Sci, 2023, 31(Suppl.):92-99
- Chloramphenicol is a bacteriostatic antimicrobial.
- Shuang Luo, .et al. , Nat Commun, 2024, 15: 3780
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cytochrome P4503A4 inhibitor
Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
- Action of clotrimazole is against the division and growing of fungi.Clotrimazole alters the permeability of the fungal cell wall and inhibits the activity of enzymes within the cell. It specifically inhibits the biosynthesis of ergosterol and other sterols required for cell membrane production.
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Iron chelator
Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.- Céline Moison, .et al. , Sci Adv, 2024, Mar 22;10(12):eadl4018 PMID: 38517966
- Jamie L. Dombach, .et al. , PLoS Pathog, 2020, Dec; 16(12): e1009119 PMID: 33290418
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CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. - Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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P450 inhibitor
As an antifungal, ketoconazole is structurally similar to imidazole, and interferes with the fungal synthesis of ergosterol, a constituent of fungal cell membranes, as well as certain enzymes. - Methoxsalen (8-Methoxypsoralen) is a potent tricyclic furocoumarin suicide inhibitor of CYP (cytochrome P-450).
- Naringenin is a flavanone, a type of flavonoid, that is considered to have a bioactive effect on human health as antioxidant, free radical scavenger, anti-inflammatory, carbohydrate metabolism promoter, and immune system modulator.
- Tong Pan, .et al. , Life Sci, 2024, Mar 1:340:122453 PMID: 38272439
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TXAS inhibitor
Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM. -
CYP3A4 inhibitor
Posaconazole is an inhibitor primarily of CYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor of sterol C14?? demethylase inhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 15-35 hours. - Sodium danshensu is a sodium salt of danshensu from the widely used Chinese herb Danshen (Salvia miltiorrhiza Bunge). In vitro and in vivo studies revealed that danshensu possessed diverse pharmacological effects, including relaxation of coronary artery, anticoagulation, protection of myocardial ischemia-reperfusion injury, and antiarrhythmia activities
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CYP17 inhibitor
Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion. -
CYP17A1 inhibitor
TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme. -
CYP17 inhibitor
Abiraterone acetate (CB7630) is an orally active acetate ester of the steroidal compound Abiraterone with antiandrogen activity. Abiraterone inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1). -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. - TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.
- Anirudh Sattiraju, .et al. , Immunity, 2023, Aug 8;56(8):1825-1843 PMID: 37451265
- Anirudh Sattiraju, .et al. , bioRxiv, 2022, March 04
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CYP3A Inhibitor
Cobicistat is a potent inhibitor of cytochrome P450 3A enzymes, including the important CYP3A4 subtype. It also inhibits intestinal transport proteins, increasing the overall absorption of several HIV medications, including atazanavir, darunavir and tenofovir alafenamide fumarate. -
Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. - Luliconazole is an azole antifungal indicated for the topical treatment of interdigital tinea pedis.
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anti-inflammatory corticosteroid
Clobetasol propionate is a anti-inflammatory corticosteroid used to treat various skin disorders. - Hydroxyflutamide (Hydroxyniphtholide) is a metabolite of flutamide found to inhibit the proliferation of estradiol-induced growth of MCF-7 breast cancer cells.
- Ren X, .et al. , Biochem Pharmacol, 2017, Sep 15;140:73-88 PMID: 28642037
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CYP3A4 inhibitor
PF 4981517 is a potent and selective inhibitor of CYP3A4 (IC50 values are 0.03, 17 and 70 μM for CYP3A4, CYP3A5 and CYP3A7 respectively). -
CYP17 inhibitor
CYP17-IN-1 (compound 9c) is a potent and orally active CYP17 inhibitor against rat and human CYP17 with IC50s of 15.8 and 20.1 nM. -
Cytochrome P450 inhibitor
Talarozole R enantiomer inhibits the metabolism of retinoic acid by blocking the cytochrome P450 enzyme isoform CYP26, a retinoic acid hydroxylase. -
Fluorescent P450 substrate
3-Cyano-7-ethoxycoumarin is a fluorogenic substrate suitable for the continuous determination of cytochrome P450 mixed-function monooxygenases. It is a fluorescent probe useful in microsomal dealkylase studies. -
cytochrome P450 substrate
Methoxyresorufin is a fluorometric substrate for cytochrome P450 linked enzymes.