NSC228155CAS号: 113104-25-9分子式: C11H6N4O4S分子量: 290.25描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)
产品描述 | |
描述 |
NSC228155 is an activator of EGFR, binding to the sEGFR dimerization domain II and modulate EGFR tyrosine phosphorylation. |
纯度 |
>98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
NSC-228155;NSC 228155
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外观 |
棕黄色固体
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可溶性/溶解性 |
DMSO : 16 mg/mL (55.12 mM; Need ultrasonic)
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生物活性 | |
靶点 |
EGFR,KIX-KID
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In vitro(体外研究) |
Previous study found that NSC228155 could dose-dependently inhibit KIX–KID interaction as measured by the split RLuc assay. In living HEK 293T cells, NSC228155 could inhibit CREB-mediated gene transcription with an IC50 of 2.09 μM. NSC228155 also inhibited VP16-CREB-mediated gene transcription with an IC50 of 6.14 μM. Though this was around 3-fold higher than the IC50 of CREB-mediated gene transcription, such results indicated that NSC228155 was not particularly selective in inhibiting KIX–KID interaction inside these living cells. Therefore, although NSC228155 was a potent inhibitor of KIX-KID interaction, it was not selective against CREB-mediated gene transcription, and further SAR studies identified a 4-aniline substituted analog displaying a higher selectivity index.
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分子结构图