NSC-60339

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Chemical Structure| 70-09-7 同义名 : -
CAS号 : 70-09-7
货号 : A1329235
分子式 : C26H23ClN6O2
纯度 : 99%+
分子量 : 486.95
MDL号 : MFCD00866352
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

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

DMSO: 4 mg/mL(8.21 mM)，配合低频超声助溶，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 In Gram-negative bacteria, efflux pumps are able to prevent effective cellular concentrations from being achieved for a number of antibiotics[2]. NSC-60339, a polybasic terephthalic acid derivative, is an efflux pump inhibitor and a substrate of AcrAB-TolC, currently studied as a potential cancer chemotherapeutic agent[3]. In WT-Pore cells, treatment with NSC-60339 resulted in an observed MIC (minimum inhibitory concentration) of 25 μM in the presence of novobiocin. Furthermore, NSC-60339 dramatically reduced the rate of efflux of a known AcrAB-TolC substrate, bisbenzamide dye H-33342 (HT), in E. coli cells[2].
作用机制 NSC-60339 binds to AcrA[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.05mL

0.41mL

0.21mL

10.27mL

2.05mL

1.03mL

20.54mL

4.11mL

2.05mL
参考文献

[1]Yesair DW, Kohner FA, Rogers WI, Baronowsky PE, Kensler CJ. Relationship of phthalanilide-lipid complexes to uptake and retention of 2-chloro-4',4"-di(2-imidazolin-2-yl)terephthalanilide (NSC 60339) by sensitive and resistant P388 leukemia cells. Cancer Res. 1966;26(2):202-207.

[2]Haynes KM, et al. Identification and Structure-Activity Relationships of Novel Compounds that Potentiate the Activities of Antibiotics in Escherichia coli. J Med Chem. 2017 Jul 27;60(14):6205-6219

[3]Yesair DW, et al. The retention or efflux of phthalanilide (NSC 60339)-lipid complexes by sensitive or resistant murine tumor cells and Escherichia coli B. Cancer Res. 1968 Feb;28(2):314-9