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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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). -
FGFR/CYP Inhibitor
FGFR-IN-10 is an orally bioactive inhibitor targeting fibroblast growth factor receptors (FGFR) and various cytochrome P450 enzymes (CYPs). It demonstrates significant potency against both wild type and V564F mutant FGFR2, with IC50 values of 104.1 nM and 43.6 nM, respectively. Additionally, FGFR-IN-10 inhibits CYP enzymes, including CYP2C9 (IC50: 3.33 µM), CYP2C19 (IC50: 18.75 µM), CYP2D6 (IC50: 4.34 µM), and CYP3A4 (IC50: 0.69 µM). This compound is valuable for researching FGFR-related signaling pathways and the pharmacokinetics of drug metabolism. -
CypA 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. -
CYP450 ω-Hydroxylase Inhibitor
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. -
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. -
CYP3A4 Inhibitor
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. -
Fungal CYP51 Inhibitor
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 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. -
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. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-2 is a quinazoline compound that functions as a dual inhibitor of CYP51 and PD-L1, exhibiting IC50 values of 0.263 μM and 0.017 μM, respectively. It displays notable antifungal activity by triggering early apoptosis in fungal cells, leading to significant reductions in intracellular IL-2, NLRP3, and NF-κBp65 protein levels. Additionally, CYP51/PD-L1-IN-2 induces mitochondrial damage and reactive oxygen species (ROS) accumulation, culminating in fungal lysis and subsequent cell death. This compound is valuable for research exploring antifungal mechanisms and cancer immunotherapy. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-1 is a dual inhibitor targeting both CYP51 and PD-L1, exhibiting an IC50 of 0.884 μM for CYP51 and 0.083 μM for PD-L1. This quinazoline compound demonstrates notable antifungal activity by inducing early apoptosis in fungal cells while significantly reducing intracellular levels of IL-2, NLRP3, and NF-κBp65. Additionally, CYP51/PD-L1-IN-1 contributes to mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately leading to fungal lysis and cell death. This compound is valuable for research focused on antifungal therapies and immune modulation. -
CYP51 Inhibitor
CYP51-IN-19 is a potent inhibitor of cytochrome P450 51 (CYP51), a critical enzyme involved in sterol biosynthesis in fungi. This compound induces the generation of reactive oxygen species (ROS), leading to significant fungicidal activity. It is primarily utilized in antifungal research and the development of therapeutic agents targeting fungal infections. -
CYP1A2 Inhibitor
Frutinone A is a selective inhibitor of CYP1A2, featuring a chromonocoumarin structural scaffold. This compound exhibits notable antibacterial and antioxidant activities, making it a valuable tool for research in pharmacology and toxicology. Its ability to modulate the activity of CYP1A2 underscores its potential for studying drug metabolism and interactions. -
CYP3A Inhibitor
Troleandomycin, a macrolide antibiotic, functions as a selective inhibitor of the cytochrome P450 enzyme CYP3A. This compound is primarily used in research to investigate drug metabolism and interactions related to CYP3A. Additionally, it has applications in studies involving corticosteroids for conditions such as asthma, providing insights into therapeutic efficacy and safety profiles. -
JNK/CYP Inhibitor
JNK-IN-14 is a potent inhibitor of the c-Jun N-terminal kinase (JNK) family, demonstrating IC50 values of 1.81 nM for JNK1, 12.7 nM for JNK2, and 10.5 nM for JNK3. This compound effectively induces early apoptosis and causes cell cycle arrest in the G2/M phase. Additionally, JNK-IN-14 exhibits a modest inhibition of beclin-1 expression in K562 leukemia cells, indicating its potential application in cancer research and therapeutic strategies targeting JNK signaling pathways. -
GSK3β Inhibitor
GSK3β-IN-3 is an ATP-competitive inhibitor of glycogen synthase kinase 3 beta (GSK3β), exhibiting an IC50 of 0.90 μM. It effectively lowers the phosphorylation levels of tau protein in the BR5706 strain and reduces the accumulation of amyloid-beta (Aβ) aggregates in the CL2006 strain. This compound is essential for research applications focused on Alzheimer's disease (AD), aiding in the understanding of neurodegenerative mechanisms and potential therapeutic strategies. -
Cytochrome P450 Inhibitor
Kushenol K is a flavonoid antioxidant derived from the roots of Sophora flavescens, functioning as a selective inhibitor of cytochrome P450 3A4 (CYP3A4) with a Ki value of 1.35 μM. This compound exhibits weak antiviral activity against herpes simplex virus type 2 (HSV-2) with an EC50 of 147 μM. Additionally, Kushenol K inhibits sodium-glucose co-transporters SGLT1 and SGLT2, making it relevant for research in metabolic disorders and viral infections. -
CYP51 Inhibitor
Obtusifoliol is a selective inhibitor of cytochrome P450 51 (CYP51), demonstrating affinities with dissociation constants (Kd) of 1.2 μM for Trypanosoma brucei and 1.4 μM for human CYP51. This compound is significant in studies focused on trypanosomiasis, targeting the sterol biosynthesis pathway. Its inhibition of CYP51 may provide valuable insights into therapeutic strategies against related infections and contribute to the understanding of cholesterol metabolism in various biological systems. -
CYP3A4 Inhibitor
SR9186 is a selective inhibitor of CYP3A4, demonstrating potent inhibition with IC50 values of 9 nM for the metabolism of Midazolam, 4 nM for Testosterone, and 38 nM for Vincristine. This compound effectively impedes hepatic-stage P. falciparum development and obstructs the metabolism of ivermectin. Its utility extends to breast cancer research, making it a valuable tool for investigating drug metabolism and therapeutic applications. -
CypD Inhibitor
CypD-IN-5 is a selective inhibitor of cyclophilin D (CypD), a key regulator of mitochondrial permeability transition. This compound demonstrates significant potential in modulating mitochondrial function and may be particularly useful in studying neurodegenerative diseases such as Alzheimer's disease. Its application in research focuses on understanding the role of CypD in cellular stress responses and the underlying mechanisms of neurodegeneration. -
CYP3A Inhibitor
ALT-2074 is a CYP3A inhibitor with an IC50 value ranging from 2.0 to 2.6 μM, functioning as a catalytic analogue of glutathione peroxidase. Although it demonstrates a weak inhibitory effect on CYP3A in vivo, it serves as a valuable tool for studying the role of oxidative stress in inflammatory diseases, including acute coronary syndrome. This compound is particularly useful in research investigating the interplay between reactive oxygen species and metabolic pathways. -
CYP51 Inhibitor
VNI is a potent inhibitor of cytochrome P450 51 (CYP51), targeting sterol synthesis in the parasite Trypanosoma cruzi. Its mechanism of action disrupts the biosynthesis of essential sterols, leading to impaired growth and viability of the pathogen. VNI is primarily utilized in research focused on anti-parasitic strategies and the development of therapeutics for Chagas disease. -
CYP51 Inhibitor
CYP51-IN-15 is a selective inhibitor of CYP51, targeting the enzyme in Naegleria fowleri. With an EC50 value of 1.5 μM, it demonstrates potent biological activity against this pathogenic organism. This compound is valuable in research aimed at elucidating mechanisms of action and developing therapeutic strategies against Naegleria fowleri infections. -
CYP51 Inhibitor
LP8 is a pyridinyl-type inhibitor of cytochrome P450 51 (CYP51), specifically targeting the sterol biosynthesis pathway in various pathogens. This compound exhibits significant biological activity against Trypanosoma cruzi, the causative agent of Chagas disease and American trypanosomiasis. LP8 is valuable for research applications aimed at elucidating the mechanisms of these diseases and developing potential therapeutic strategies. -
CYP3A Inhibitor
Cobicistat-d8 is a deuterated analog of Cobicistat, acting as a potent and selective inhibitor of cytochrome P450 3A (CYP3A) with IC50 values ranging from 30 to 285 nM. This reagent functions primarily as a pharmacokinetic enhancer, improving the absorption and bioavailability of anti-HIV agents. Its role in modulating drug metabolism makes it a valuable tool in pharmaceutical research and drug development. -
CYP1A1 Inhibitor
CYP1A1-IN-1 is a selective inhibitor of cytochrome P4501A1 (CYP1A1). This compound has demonstrated the ability to reduce bacterial loads of methicillin-resistant Staphylococcus aureus (MRSA) and Acinetobacter baumannii through the enhancement of macrophage phagocytosis. CYP1A1-IN-1 holds potential for advancing research in sepsis associated with multidrug-resistant (MDR) bacterial infections. -
CYP2C1/CYP2C19 Inhibitor
CYP2C1/CYP2C19-IN-2 is a potent inhibitor of the CYP2C1 and CYP2C19 enzymes. This compound exhibits minimal hepatotoxicity and lacks Ames toxicity, making it a safer choice for research applications. CYP2C1/CYP2C19-IN-2 is particularly useful in studies investigating antiviral mechanisms against Zika virus (ZIKV). -
CYP2C9/CYP2C19 Inhibitor
CYP2C9/CYP2C19-IN-1 is a potent inhibitor of the cytochrome P450 enzymes CYP2C9 and CYP2C19. This compound exhibits key biological activity by effectively modulating drug metabolism pathways without hepatotoxic effects or Ames toxicity. It serves as a valuable tool for research applications, including studies on anti-Zika virus (ZIKV) therapeutics. -
CYP17A1 Inhibitor
YM116 is a potent and orally active competitive inhibitor of CYP17A1, with a reported Ki of 0.38 nM. By specifically inhibiting the C17-20 lyase activity, YM116 effectively reduces the synthesis of adrenal androgens, leading to decreased serum testosterone levels and lower dehydroepiandrosterone sulfate concentrations. This compound is valuable for research applications involving androgen-related disorders and prostate health. -
hCYP3A4 Inhibitor
hCYP3A4-IN-1 is a potent inhibitor of human cytochrome P450 3A4 (hCYP3A4) with notable activity in both human liver microsomes and CHO-3A4 stable cell lines, exhibiting IC50 values of 43.93 nM and 153.00 nM, respectively. This inhibitor effectively blocks CYP3A4-mediated hydroxylation of N-ethyl-1,8-naphthalimide (NEN) in a competitive manner, with a Ki of 30.00 nM. hCYP3A4-IN-1 is valuable for research applications focused on drug metabolism and interactions involving CYP3A4. -
CYP3A4 Inhibitor
Tabimorelin hemifumarate is a potent inhibitor of the cytochrome P450 enzyme CYP3A4. This compound functions as a growth hormone secretagogue, promoting the secretion of growth hormone in the body. Its key biological activities make it valuable for research applications in endocrine signaling and pharmacokinetics, particularly in studies assessing drug metabolism and interactions involving CYP3A4. -
CYP4A Hydroxylase Inhibitor
CAY 10434 is a potent inhibitor of CYP4A hydroxylase, demonstrating significant effects on vascular smooth muscle contractility. This compound enhances the contractile response to angiotensin II, achieving a maximal contractile response (Emax) of 6764 mg. CAY 10434 is valuable for research into cardiovascular physiology and the regulatory mechanisms underlying vascular reactivity. -
CYP11B2 Inhibitor
CYP11B2-IN-3 is a selective inhibitor of CYP11B2, demonstrating an IC50 value of 12.92 nM for CYP11B2 and 2341 nM for CYP11B1. This compound is orally active, making it suitable for in vivo studies. CYP11B2-IN-3 is primarily applicable in research related to hypertension, providing a valuable tool for investigating the role of CYP11B2 in adrenal steroidogenesis and blood pressure regulation. -
CYP1A2/CYP2D6/CYP3A4 Inhibitor
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM, while functioning as a competitive inhibitor of CYP1A2 and CYP2D6, with Ki values of 3.39 μM and 6.77 μM, respectively. This compound plays a significant role in pharmacological research by modulating drug metabolism pathways. Its ability to inhibit key cytochrome P450 enzymes makes it a valuable tool for studies examining drug interactions and metabolic regulation. -
CYP3A4 Inhibitor
Licopyranocoumarin is an isoflavonoid known for its inhibitory action on the cytochrome P450 enzyme CYP3A4, exhibiting an IC50 of 32 μM. This compound also demonstrates significant neuroprotective properties, making it a valuable reagent for studies focused on drug metabolism and neurodegenerative disorders. Researchers may utilize Licopyranocoumarin to explore its effects on enzyme activity and potential therapeutic applications in neurological research. -
CYP1B1 Inhibitor
CYP1B1-IN-1 is a selective inhibitor of cytochrome P450 1B1 (CYP1B1) with an IC50 value of 0.49 nM. This compound is valuable for studying the role of CYP1B1 in various biological processes, including the metabolism of xenobiotics and the activation of pro-carcinogens. CYP1B1-IN-1 is suitable for research applications focused on cancer biology and toxicology, providing insights into the pharmacological modulation of CYP1B1 activity. -
CYP450 Inhibitor
11-HETE (11-Hydroxy-5,8,12,14-eicosatetraenoic acid) serves as an activator for cytochrome P450 enzymes. This compound is known to upregulate the mRNA expressions of CYP1B1, CYP1A1, CYP4A11, CYP4F11, and CYP4F2, leading to significant biological effects such as cell hypertrophy in RL-14 cells. Due to its modulatory role in cytochrome P450 activity, 11-HETE holds potential applications in the study of cardiovascular diseases. -
CYP17A1 Lyase Inhibitor
BMS-351 is a potent, orally active nonsteroidal inhibitor of CYP17A1 lyase, demonstrating IC50 values of 19 nM for human CYP17A1 and 4 nM for cynomolgus monkey CYP17A1. This compound is primarily utilized in research focused on castration-resistant prostate cancer, providing insights into hormonal regulation and potential therapeutic interventions in this challenging malignancy. -
CYP1B1 Inhibitor
(E/Z)-DMU2105 is a selective inhibitor of CYP1B1, demonstrating potent inhibition with an IC50 value of 10 nM in yeast-derived microsomes and 63.65 nM in live recombinant yeast and human HEK293 kidney cells. This compound is valuable for research focused on cancer, glaucoma, ischemia, and obesity, offering insights into the role of CYP1B1 in various biological processes. Its specificity and potency make it a suitable tool for elucidating the function of this key enzyme in disease contexts.
