KS176

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Chemical Structure| 1253452-78-6 同义名 : -
CAS号 : 1253452-78-6
货号 : A578694
分子式 : C22H19N3O5
纯度 : 99%+
分子量 : 405.4
MDL号 : MFCD22666402
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(86.33 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
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
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

[1]Pick A, Klinkhammer W, et al. Specific inhibitors of the breast cancer resistance protein (BCRP). ChemMedChem. 2010 Sep 3;5(9):1498-505.

[2]Pick A, Klinkhammer W, Wiese M. Specific inhibitors of the breast cancer resistance protein (BCRP). ChemMedChem. 2010;5(9):1498-1505. doi:10.1002/cmdc.201000216