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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.
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.
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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.
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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.
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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.
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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.
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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.
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.
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.
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17-ODYA is a selective CYP450 ω-hydroxylase inhibitor, demonstrating potent inhibition (IC50
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.
Antifungal agent 136 is an irreversible inhibitor of fungal lanosterol 14α-demethylase (CYP51). It demonstrates potent antifungal activity against drug-resistant strains of Candida albicans and effectively downregulates IL-6 expression. This compound holds potential for research applications in the fields of fungal infection and inflammatory diseases.
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.
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Uniconazole, a selective inhibitor of cytochrome P450 enzymes, primarily targets ABA 8’-hydroxylase, exhibiting an IC50 of 68 nM. This compound serves as a competitive inhibitor of CYP707A3 with a Ki value of 8 nM. Uniconazole effectively inhibits gibberellin and, to a lesser extent, brassinosteroid biosynthesis, making it a valuable tool in studies of plant growth regulation and developmental processes. Its application extends to research exploring the modulation of plant hormones.
Benzylmethyl ether is a derivative of benzyl alcohol and functions as an inhibitor of the P450 enzyme. This aromatic ether, characterized by its colorless appearance and mild aromatic odor, demonstrates significant anti-inflammatory activity. Research indicates that benzylmethyl ether modulates Toll-Like Receptor 4, effectively reducing liver injury-related inflammation in murine models, making it valuable for studies in hepatotoxicity and inflammation.
CYP51/PD-L1-IN-4 is a potent dual-target inhibitor of CYP51 and PD-L1, demonstrating IC50 values of 0.17 μM and 0.021 μM, respectively. This compound exhibits significant antifungal activity and is effective against drug-resistant fungal strains in vitro. CYP51/PD-L1-IN-4 is suitable for research applications focused on fungal infections and the interplay between fungal pathogens and immune checkpoint regulation.
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Friedelin is a non-competitive inhibitor of cytochrome P450 3A4 (CYP3A4), exhibiting IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Additionally, it acts as a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin is valuable for research applications in areas such as inflammation, neurological diseases, and metabolic disorders, providing insights into the modulation of these critical pathways.
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).
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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.
Synonyms: HZIV 81-2
Tetrahydrocurcumin is a cytochrome P450 inhibitor derived from the reduction of curcumin, a principal component of turmeric (Curcuma longa). This compound selectively inhibits CYP2C9 and CYP3A4 activity, making it a valuable tool for studies investigating drug metabolism and interactions. Its biological activity contributes to research in pharmacology and toxicology, particularly in the context of enhancing understanding of metabolic pathways.
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.
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.
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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.
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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.
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Synonyms: Resorufin ethyl ether
7-Ethoxyresorufin is a fluorometric substrate and competitive inhibitor of cytochrome P450, with a notable specificity for CYP1A1. This compound is utilized in studies related to xenobiotic metabolism and drug interactions, providing essential insights into cytochrome P450 enzyme activity. Additionally, 7-Ethoxyresorufin has been shown to inhibit nitric oxide synthase, facilitating research on nitric oxide signaling pathways.
