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编 号:F506967
分子式:C16H14N2O2
分子量:266.29
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生物活性:
Inz-1 is a potent and selective mitochondrial cytochrome bc1 inhibitor for yeast (IC50=8.092 μM) over humans (IC50=45.320 μM). Inz-1 reverses Fluconazole (HY-B0101) or other triazole antifungals’ resistance in?the pathogenic fungus Candida albicans.

体外研究:
Inz-1 (0-16 μM; 24 hours) inhibits the growth of the model yeast?S. cerevisiae?(strain BY4741) and?C. albicans?(SC5314) in media containing glucose or glycerol as the sole carbon source, while only mildly slowing growth in glucose.?Inz-1 (0-100 μM; 24 hours) shows inhibition of yeast cytochrome B enzymatic activity in a concentration -dependent manner in both wild-type and F90Y mutant mitochondria. It exhibits inhibition of cytochrome bc1 from both?S. cerevisiae and?C. albicans?with IC50 value of 2.5 μM and 8.0 μM, respectively.Inz-1 (0-100 μM; 24 hours) is selective for yeast over human cytochrome bc1, it inhibits human cytochrome bc1 activity only weakly, with an IC50?of 45.3 μM, 5.6-fold higher than the IC50?for the?C. albicans?homolog in mitochondria purified from HEK293 human embryonic kidney cells.Inz-1 (0-100 μM; 24 hours) inhibits proliferation under forced respiration conditions only at 32 μM,and only mildly at that concentration.Inz-1 is against candida, human enzyme with IC50 values of 8.092μM and 45.320 μM, respectively. It against Candida and HepG2 respiring growth with IC50 values of 1.655 uM and >32 μM, respectively.
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