cyp24a1

Ketoconazole (R-41400) is an imidazole antifungal agent with broad-spectrum antifungal activity that primarily acts by inhibiting the biosynthesis of ergosterol in the fungal cell membrane. Ketoconazole inhibits the fungal cytochrome P450-dependent enzyme lanosterol 14α-demethylase (CYP51), thereby blocking the conversion of lanosterol to ergosterol. This leads to damage to the cell membrane structure and permeability, consequently inhibiting fungal growth and producing an antifungal effect. In addition, ketoconazole is a non-selective cytochrome P450 (CYP) inhibitor, specifically inhibiting drug-metabolizing enzymes such as human CYP3A4. In terms of endocrinology, ketoconazole also inhibits various enzymes involved in steroid synthesis (CYP17A1, CYP11A1).

SDZ285428 is a CYP24A1 inhibitor.

(-)-Ketoconazole is a potential mitochondrial CYP24A1 inhibitor and has antifungal activity against Aspergillus fumigatus.

AC-340 is a potent hybrid molecule functioning as a VDR agonist and HDAC inhibitor. It can significantly induce the expression of VDR target genes such as CYP24A1, with a selectivity for HDAC2 approximately 10 times greater than for HDAC6 (IC50= 0.37 μM). By causing extensive protein hyperacetylation, such as that of tubulin and H3K9/K27, AC-340 enhances VDR superagonism, resulting in increased acetylation levels of H3K27 on VDR target genes. AC-340 is applicable in research related to melanoma.

(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3), a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3), exerts potent actions through vitamin D receptor (VDR) activation, including the inhibition of keratinocyte growth and suppression of parathyroid hormone secretion [1].