Cytochrome P450

TH-302 is a selectively targeting hypoxic regions of solid tumors hypoxia-activated prodrug.

Deferasirox is a rationally-designed oral iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor.

Clarithromycin is a macrolide antibiotic. It prevents bacteria from growing by interfering with their protein synthesis.

Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17,20 lyase (CYP17A1), an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues.

Itraconazole is a relatively potent inhibitor of CYP3A4 with IC50 of 6.1 nM, used as a triazole antifungal agent.

Hydroxyflutamide (Hydroxyniphtholide) is a metabolite of flutamide found to inhibit the proliferation of estradiol-induced growth of MCF-7 breast cancer cells.

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.

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.

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.

Chloramphenicol is a bacteriostatic antimicrobial.

Avasimibe (CI-1011) is an orally bioavailable Acyl-CoA:Cholesterol O-Acyltransferase (ACAT) 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.

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.

Haloperidol (Haldol) is an antipsychotic and butyrophenone.

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).

Ozagrel is a potent and selective thromboxane A2 synthetase inhibitor with an IC50 of 4 nM.

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

Voriconazole (Vfend) is a triazole antifungal agent that is available as a lyophilized powder for solution for intravenous infusion.

TAK-700 (Orteronel) is an oral, non-steroidal androgen synthesis inhibitor that selectively inhibits the 17,20 lyase enzyme.

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).

SDZ285428 is a CYP51 inhibitor.

HL001 is an oral small molecule inhibitor targeting Cyclophilin A (CypA) and acting as a receptor antagonist for Lysophosphatidic acid 1 (LPA1). This compound induces cell cycle arrest and apoptosis in tumor cells via p53 stabilization, achieved by down-regulating G3BP1 and promoting reactive oxygen species production and DNA damage. HL001 disrupts the MDM2-p53-72R interaction in a CypA-dependent manner, demonstrating significant antitumor activity. Additionally, HL001 serves as a valuable tool in the investigation of pulmonary fibrosis.

17-ODYA is a selective CYP450 ω-hydroxylase inhibitor, demonstrating potent inhibition (IC50<100 nM) of 20-hydroxyeicosatetraenoic acid (20-HETE) and related eicosanoids in rat renal cortical microsomes. This compound effectively prevents isoproterenol-induced apoptosis and necrosis in cultured cardiomyocytes. Additionally, 17-ODYA serves as a click chemistry reagent with an alkyne group, facilitating copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules, making it a valuable tool for various biochemical applications.

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.

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.

Escholtzine perchlorate is a potent CYP3A4 inhibitor derived from the alkaloid Eschscholzia californica. This compound demonstrates significant biological activity, with an IC50 value for CYP3A4 of 13.4 μM and an EC50 value for the 5-HT1A receptor of 11 μM. Escholtzine perchlorate is primarily utilized in research focused on anxiety and depression, offering valuable insights into pharmacological mechanisms related to these conditions.

VT-1598 is an orally active and selective inhibitor of fungal cytochrome P450 51 (CYP51). It exhibits potent antifungal activity against Candida auris, making it a valuable tool for research into fungal infections. Additionally, VT-1598 contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry applications, facilitating the study of various biological interactions.

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.

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.

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.

(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.

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.

Pipercroside A is a potent CYP51 inhibitor derived from Piper crocatum Ruiz & Pav. This compound exhibits significant antifungal activity, making it a valuable tool in studies of fungal infections and drug resistance mechanisms. Its role in inhibiting sterol biosynthesis positions Pipercroside A as a candidate for further investigation in antifungal therapeutic development.

Pipercroside B is a potent inhibitor of CYP51, an essential enzyme in sterol biosynthesis. Isolated from Piper crocatum Ruiz & Pav, this compound exhibits significant antifungal activity, making it valuable for research into antifungal therapeutics. Its role in modulating CYP51 provides insights into fungal metabolism and potential treatment strategies against fungal infections.