Catalog No.
Product Name
Application
Product Information
Citations
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CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
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. - Chlorzoxazone is a muscle-relaxing drug,and a probe for human liver cytochrome P-450IIE1.
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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. -
human cytochrome P450IA2 inhibitor
Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with an IC50 of 0.07 μM. -
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). - Phortress, also known as NSC-710305 and 5F-DF-203-L-lysinamide, is a P450 CYP1A1-activated antitumor prodrug with antitumor activity. Phortress free base leads to DNA damage and cell cycle arrest.
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EMT inhibitor
EMT inhibitor-2 inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively. -
fungal Cyp51 inhibitor
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes. - Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).
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Cytochrome P450 inhibitor
4'-Methylchrysoeriol is a potent inhibitor of Cytochrome P450 enzymes, with an IC50 of 19 nM for human P450 1B1-dependent EROD. -
peptidoleukotrienes antagonist
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M. -
cytochrome P450 1B1 inhibitor
1-Ethynylnaphthalene is a selective inhibitor of cytochrome P450 1B1. -
CYP51 inhibitor
Oteseconazole (VT-1161) is an orally active anti-fungal agent, potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM), shows no obvious effect on human CYP51. -
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). -
CYP17 lyase inhibitor
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. -
CYP26 inhibitor/RAMBA
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. -
liver CYP3A4 substrate
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM. -
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. - Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
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anti-inflammatory agent
Cepharanthine is an alkaloid derived from Stephania cepharantha Hayata, with possesses anti-inflammatory and antioxidative activities. -
CYP3A4 inducer
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 ?l/min per mg protein and uptake and biliary clearances of 2.6 and 1.6 ?l/min per mg protein, respectively. -
Cholesterol 24-hydroxylase (CH24H) inhibitor
Soticlestat, also known as TAK 935 and OV935, is an inhibitor of the enzyme cholesterol 24-hydroxylase (CH24H). -
20-HETE synthase inhibitor
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 Inhibitor
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 Inhibitor
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 Inhibitor
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 Inhibitor
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. -
CYP51 Inhibitor
(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. -
Fungal CYP51A1 Inh
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. -
CYP51 Inhibitor
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. -
CYP51 Inhibitor
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. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-3 is a dual inhibitor targeting CYP51 and PD-L1, exhibiting potent antifungal activity with IC50 values of 0.205 μM and 0.039 μM, respectively. This compound induces early apoptosis in fungal cells by reducing levels of intracellular IL-2, NLRP3, and NF-κBp65 proteins. Additionally, CYP51/PD-L1-IN-3 causes mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately resulting in fungal lysis and cell death. This compound serves as a valuable tool for research in fungal infections and immune modulation.
