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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. -
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
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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
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CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
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. -
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. -
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. -
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. -
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). -
XOR Inhibitor
Topiroxostat (FYX-051) is a novel and potent xanthine oxidoreductase (XOR) inhibitor with IC50 value of 5.3 nM. -
CYP3A4 Inhibitor
Azithromycin, derived from erythromycin, is a antibiotic. Azithromycin binds to the 50S subunit of the bacterial ribosome, and thus inhibits translation of mRNA. -
CYP2C19/CYP2B6 inhibitor
Choline Fenofibrate (ABT-335) is the choline salt of fenofibric acid under clinical development as a combination therapy with rosuvastatin for the management of dyslipidemia. -
CYP2C9 inhibitor
Benzbromarone is a CYP2C9 inhibitor, it binds to CYP2C9 with Ki value of 19.3 nM. -
CYP1A1 inhibitor
Bergamottin is a furanocoumarin found in grapefruit juice and lemon, lime, and bergamot oils that has diverse biological activities. -
CYP51 inhibitor
Tebuconazole is a triazole fungicide used agriculturally to treat plant pathogenic fungi. -
CYP2C9 inhibitor
Sulfaphenazole is a specific inhibitor of CYP2C9 which blocks atherogenic and pro-inflammatory effects of linoleic acid (increase in oxidative stress and activation of AP-1) mediated by CYP2C9. -
Cytochrome P450 inhibitor
Proadifen hydrochloride is a Cytochrome P450 inhibitor (IC50 = 19μM). -
cytochrome P450 1B1 inhibitor
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. -
DAF-9 cytochrome P450 inhibitor
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1). -
CYP450 dependent inhibitor
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). -
Cytochrome P450 hibitor
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 ?M and 22.8 ?M for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects. -
Cholesterol 24-hydroxylase (CH24H) inhibitor
Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H).
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