生物活性 | |||
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描述 | Breast cancer resistance protein (BCRP) plays an important role in the development of multidrug resistance. KS176 is a potent and selective BCRP inhibitor with IC50 values of 1.39±0.26 and 0.59±0.24μM in Hoechst 33342 assay and Pheophorbide A assay, respectively. It shows no activity against P-glycoprotein or multidrug resistance-associated protein 1. The inhibitory potency of KS176 against BCRP was ~50-fold more potent than novobiocin and was only slightly less than that of Ko143. KS176 did not decrease cell viability in A2780 and MCF-7 cells at concentrations up to 10μM.[2] | ||
作用机制 | KS176 is an inhibitor of BCRP. It undergoes noncompetitive interaction with pheophorbide A.[2] |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.33mL 2.47mL 1.23mL |
24.67mL 4.93mL 2.47mL |
参考文献 |
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