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NSC228155
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
NSC228155图片
CAS NO:113104-25-9
包装与价格：
包装价格(元)
10mg电议
50mg电议
100mg电议
500mg电议
1g电议

产品介绍
NSC228155 是 EGFR 的激活剂，与 EGFR 的细胞外区域结合并增强 EGFR 的酪氨酸磷酸化。 NSC228155 也是一种有效的 KIX-KID 相互作用抑制剂，抑制 CREB \u200b\u200b的激酶诱导域 (KID) 和 CBP 的 KID 相互作用域 (KIX)，IC50 为 0.36 μM。
Cas No.113104-25-9
化学名2-((7-nitrobenzo[c][1,2,5]oxadiazol-4-yl)thio)pyridine 1-oxide
Canonical SMILES[O-][N+]1=CC=CC=C1SC2=CC=C([N+]([O-])=O)C3=NON=C32
分子式C11H6N4O4S
分子量290.25
溶解度≥ 29mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50: 0.36 μM for KIX-KID interaction

NSC228155 is a potent inhibitor of KIX-KID interaction.

Cyclic-AMP response-element binding protein (CREB) is identified as a stimulus-activated transcription factor. Its transcription activity needs its binding with CREB-binding protein (CBP) after CREB is phosphorylated at Ser133. The domains involved for CREB-CBP interaction are kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP.

In vitro: 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 [1].

In vivo: So far, there is no animal in vivo data reported.

Clinical trial: Up to now, NSC228155 is still in the preclinical development stage.

Reference:
[1] Xie F, Li BX, Broussard C, Xiao X.  Identification, synthesis and evaluation of substituted benzofurazans as inhibitors of CREB-mediated gene transcription. Bioorg Med Chem Lett. 2013 Oct 1;23(19):5371-5.