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Cytochrome P450 (CYP) inhibitors act on heme enzymes that oxidize drugs, steroids and other lipophilic compounds. The name comes from the 450 nm absorption peak of a carbon monoxide-bound pigment, described in liver microsomes in 1964. Hepatic enzymes such as CYP3A4, CYP2C9 and CYP1A2 metabolize a large share of drugs and many environmental chemicals. Other members synthesize steroid hormones, among them CYP17A1, which is required for androgen production. The P450 system can also convert chemicals into toxic or carcinogenic metabolites, which links it closely to toxicology. Abiraterone inhibits CYP17A1, while clarithromycin and itraconazole serve as CYP3A4 inhibitors in drug-interaction studies. Alizarin is listed for its inhibition of enzymes in the CYP1 family.
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD.
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1.
ODM-204 is novel nonsteroidal dual inhibitor of both androgen receptor and CYP17A1 enzyme, with IC50s of 80 nM and 22 nM, respectively.
DMU2139 is a potent and specific CYP1B1 inhibitor, with IC50s of 9 nM and 795 nM for CYP1B1 and CYP1A1, respectively.
DMU2105 is a potent and specific CYP1B1 inhibitor, with IC50s of 10 nM and 742 nM for CYP1B1 and CYP1A1, respectively.
BI 689648 is a novel, highly selective aldosterone synthase inhibitor which can inhibit CYP11B1 and CYP11B2 with IC50s of 310 and 2.1 nM, respectively.
Synonyms: VT-1161
Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd,
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).
Synonyms: VT-464
Seviteronel (VT-464) is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition.
Synonyms: INXN-1001; RG-115932
Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.
Synonyms: R115866
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
Synonyms: R75251 dihydrochloride; R 75251
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).
Synonyms: Gentiopicrin
Gentiopicroside, a naturally occurring iridoid glycoside, inhibits P450 activity, with an IC50 and a Ki of 61 µM and 22.8 µM for CYP2A6; Gentiopicroside has antianti-inflammatoryand antioxidative effects.
Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
RO6889678 is an inhibitor of HBV with a complex ADME profile. RO6889678 showed an intracellular enrichment of 78-fold in hepatocytes, with an apparent intrinsic clearance of 5.2 µl/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 µl/min per mg protein, respectively.
Synonyms: TAK-935; OV935
Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H).
HET0016 is a potent and selective inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthase, with IC50 values of 17.7 nM, 12.1 nM, and 20.6 nM for CYP4A1-, CYP4A2-, and CYP4A3-mediated 20-HETE synthesis, respectively. It also acts as a selective cytochrome P450 (CYP450) inhibitor and has been shown to suppress angiogenesis and tumor growth, making it a valuable compound for cancer and vascular research.
Synonyms: (+)-Cedrol; α-Cedrol
Cedrol is a potent competitive inhibitor of cytochrome P450 enzymes. It demonstrates significant biological activities, including inducing cell cycle arrest and caspase-dependent apoptosis, which contribute to its anticancer effects. Additionally, Cedrol acts as a neutrophil agonist, modifying cellular responses to N-formyl peptide stimulation. Its analgesic properties counteract neuropathic pain linked to chronic injuries by mitigating oxidative stress and inflammation. Moreover, Cedrol exhibits antibacterial properties and has potential applications in hair loss prevention and the management of anxiety.
CYP51/HDAC-IN-1 is a potent dual inhibitor of CYP51 and HDAC, demonstrating significant biological activity in combating virulence factors as well as down-regulating resistance-associated genes. This compound shows promising therapeutic potential for treating tropical candidiasis and cryptococcal meningitis, making it a valuable tool for research in antifungal therapies.
CYP17A1/HDAC6-IN-1 is a dual inhibitor targeting both CYP17A1 and HDAC6, exhibiting IC50 values of 0.284 μM and 0.6015 μM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology. Its ability to simultaneously inhibit these targets suggests potential applications in therapeutic strategies against malignancies driven by steroidogenesis and histone deacetylation.
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CYP51-IN-30 is a potent inhibitor of CYP51, targeting sterol 14α-demethylase, an essential enzyme in sterol biosynthesis. This compound exhibits significant fungicidal activity, demonstrated by an EC50 value of 2.97 mg/L against Sclerotinia sclerotiorum. Its efficacy makes it a valuable tool for research in antifungal studies and applications in plant pathology.
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CYP51-IN-32 is a selective inhibitor of CYP51, demonstrating a potent antifungal activity with an IC50 of 0.331 μM against Candida albicans. This compound not only inhibits the growth of Candida albicans by disrupting hyphal formation and biofilm development, but it also releases hydrogen sulfide (H2S), contributing to its antifungal effects. CYP51-IN-32 is suitable for investigating Candida albicans infections and can be formulated into PEG-based nanovesicles for enhanced delivery in research applications.
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Synonyms: (Rac)-Ketoconazol; (Rac)-R 41400
(Rac)-Ketoconazole is an imidazole antifungal agent that acts as a potent inhibitor of cytochrome P450-dependent 14α-sterol demethylase (CYP51). By disrupting ergosterol synthesis, it induces membrane dysfunction, thereby inhibiting the growth and reproduction of various fungi. This compound is primarily utilized in research relating to fungal infections and the mechanisms of antifungal resistance.
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Becliconazole functions as an inhibitor of the fungal cytochrome P450 51A1 (CYP51A1) enzyme. This compound exhibits significant antifungal activity and is primarily utilized in research related to fungal infections, offering insights into the mechanisms of action and potential therapeutic interventions against fungal pathogens.
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