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.

Tetrahydrocurcumin-d6 is a deuterated analog of Tetrahydrocurcumin, functioning as an inhibitor of CYP2C9 and CYP3A4 enzymes. This compound exhibits significant biological activity against these cytochrome P450 isoforms, making it valuable for research into drug metabolism and pharmacokinetics. Tetrahydrocurcumin-d6 is utilized in studies aiming to elucidate the metabolic pathways and interactions of curcuminoids, as well as their potential therapeutic applications.

Gemfibrozil 1-O-β-glucuronide is a competitive inhibitor of the CYP2C8 enzyme, exhibiting an IC50 of 4.07 μM. As a metabolite of Gemfibrozil, this compound plays a significant role in studying drug metabolism and interactions, particularly within the context of lipid metabolism and therapeutic drug monitoring. Its inhibition capacity makes it relevant for research focused on pharmacokinetics and the effects of CYP2C8 modulation on drug efficacy and safety.

CYP2E1-IN-1 is a potent inhibitor of cytochrome P450 2E1 (CYP2E1) with a Kd of 7.02 μM, an IC50 of 1.64 μM, and a Ki of 0.897 μM. This compound activates the Nrf2/HO-1 signaling pathway and effectively inhibits reactive oxygen species (ROS) production, contributing to the alleviation of pancreatic injury. With significant anti-inflammatory and antioxidant properties, CYP2E1-IN-1 is suitable for research applications focused on severe acute pancreatitis and other inflammation-related diseases.

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.

CYP2C19-IN-1 is a selective inhibitor of the cytochrome P450 enzyme CYP2C19, exhibiting a favorable safety profile with no hepatotoxicity or Ames test toxicity. It demonstrates potent inhibition of RNA-dependent RNA polymerase (RdRP) with a Ki value of 6.16 µM. This compound is primarily utilized in research focused on antiviral therapies against Zika virus (ZIKV).

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.

3-Methoxyphenylethylamine is a substrate for cytochrome P450 2D6 (CYP2D6), playing a crucial role in drug metabolism. It is commonly used in research to investigate the metabolic pathways and enzyme interactions involving CYP2D6, making it valuable for studies on pharmacokinetics and drug-drug interactions. Additionally, this compound serves as an important intermediate in the synthesis of pharmaceuticals and other organic materials, furthering its applications in chemical research.

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.

RPR203494 is a selective inhibitor of cytochrome P450 (CYP) isozymes, with significant activity against p38 mitogen-activated protein kinase, exhibiting an IC50 of 9 nM and an EC50 of 60 nM. This compound effectively inhibits hepatic CYP enzymes, making it a valuable tool in the study of drug metabolism and pharmacokinetics. RPR203494 holds potential for research applications related to rheumatoid arthritis and other inflammatory conditions, aiding in the exploration of therapeutic strategies targeting CYP-mediated pathways.

CYP1B1-IN-6 is a selective inhibitor of the cytochrome P450 enzyme CYP1B1. This compound demonstrates the ability to inhibit CYP1B1 activity, making it useful for tumor identification in fluorescence and photoacoustic imaging modalities. CYP1B1-IN-6 can assist in research applications focused on cancer diagnostics and the investigation of metabolic processes involving CYP1B1.

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.

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.

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.

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.

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.

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.

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-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.

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.

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-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.

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.

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.