cyp

CYP11B2-IN-1 is an effective and selective inhibitor of CYP11B2 with IC50s of 2.3 nM and 142 nM for CYP11B2 and CYP11B1.

CYP17-IN-1 is an effective oral inhibitor of CYP17 that can inhibit CYP17 in rats and humans with IC50 of 15.8 and 20.1 nM.

NP10679 is an orally available, selective, brain-penetrating, potent, and pH-sensitive N-methyl-D-aspartate (NMDA) receptor inhibitor of the GluN2B subunit.NP10679 inhibits histamine H1, hERG channels, and CYP enzymes, and may be useful in the study of epilepsy and ischemic stroke.

Bergapten (5-Methoxypsoralen), a psoralen, inhibits cell replication.

Naringin dihydrochalcone (Naringin DC) is an inhibitor of CYP enzymes, used as an artificial sweetener.

Tetrahydropiperine (Cosmoperine) is a natural product derived from piperine, can be used to treat convulsion, epilepsy, relieve pain, and control insects.

BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

Miltirone is a CYPs inhibitor, it has been characterized as a low-affinity ligand for central benzodiazepine receptors.

BL-1020 Mesylate (CYP-1020 Mesylate) is an orally available GABA A receptor agonist and D2 antagonist that decreases dopamine activity and enhances GABAA activity.BL-1020 Mesylate has been used in the study of schizophrenia, Alzheimer's disease, and bi-directional cognitive impairment.

Itraconazole (R51211) is a triazole antifungal agent that inhibits cytochrome P-450-dependent enzymes necessary for ERGOSTEROL synthesis.

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

CYP1B1-IN-1 is a selective and highly potent cytochrome P450 1B1 (CYP1B1) inhibitor with potential anticancer and antitumor activity for breast cancer research.

(2-methylpropyl)({[3-(trifluoromethyl)phenyl]methyl})amine is a selective serotonin receptor agonist that specifically targets 5-HT2A and 5-HT2C receptors. It has been used to study the role of serotonin in a variety of physiologic and pathologic conditions.

CYP1A1 inhibitor 8a is a potent and selective CYP1A1 inhibitor. It antagonizes B[a]P mediated activation of aromatic hydrocarbon receptor (AhR) in yeast cells, thereby protects human cells from CYP1A1-mediated B[a]P toxicity.

CYP4A11/CYP4F2-IN-1 is a cytochrome P450 (CYP) 4A11 and CYP4F2 inhibitor, applicable for research on kidney, cardiovascular, and cerebrovascular diseases.

PROTAC CYP1B1 Degrader-1 (Compound 6C), an α-naphthoflavone chimera derivative, effectively targets and degrades cytochrome P450 (CYP) 1B1 to overcome agent resistance, displaying half-maximal inhibitory concentrations (IC50s) of 95.1 nM for CYP1B1 and 9838.6 nM for CYP1A2. This compound is suitable for investigating prostate cancer characterized by overexpression of CYP1B1 [1].

CYP51-IN-20 (compound 5b), an antifungal agent, effectively inhibits CYP51 and exhibits significant activity against Candida albicans ATCC 10231. It suppresses the ERG11 (Cyp51) gene expression and markedly curtails the morphological transformation from yeast to hyphae. Furthermore, when combined with Voriconazole, CYP51-IN-20 synergistically occupies the entire CYP51 binding site, enhancing its inhibitory impact in the Glechoma moth model.

CYP51-IN-21 (Compound A33) is an effective inhibitor of CYP51, exhibiting excellent antifungal activity against pathogenic fungi and resistant strains. It also inhibits the formation of fungal biofilms.

CYP3A4-IN-4 (compound Δ,Λ-3) constitutes a Ru(II)-Ir(III) complex that acts as a photoactive inhibitor of the primary human drug-metabolizing enzyme CYP3A4. This complex features a [Ru(tpy)(Me2bpy)] photocaging group and exhibits an IC50 of 2.2 μM for the inhibition of microsomal CYP3A4 under irradiation conditions (λirr=530 nm, tirr=15 min). The phototherapeutic index (PI) of CYP3A4-IN-4 is 5.4.

CYP51-IN-9 (compound 1i) is an analog of Fluconazole and serves as an effective antifungal agent. It exhibits a MIC80 of 62.5 ng/mL against Microsporum gypseum and Candida albicans, indicating potent inhibitory activity.

CYP51-IN-12 (compound 1l), an analog of Fluconazole, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with a MIC80 of 15.6 ng/mL.

CYP51-IN-7 (compound 1g) is an analogue of Fluconazole and serves as an effective antifungal agent. It exhibits inhibitory activity against Microsporum gypseum and Candida albicans, with MIC80 values of 62.5 ng/mL and 250 ng/mL, respectively.

CYP51-IN-14 (compound 1n), a derivative of Fluconazole, functions as an effective antifungal agent. This compound inhibits Microsporum gypseum and Candida albicans with a minimum inhibitory concentration (MIC80) of 1 μg/mL.

CYP51-IN-13 (compound 1m), a fluconazole analog, serves as an effective antifungal agent. It inhibits Microsporum gypseum and Candida albicans with MIC80 values of 62.5 ng/mL and 250 ng/mL, respectively.