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Naphthol AS-E
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。
Naphthol AS-E图片
CAS NO:92-78-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议

产品介绍
Naphthol AS-E 是有效的，具有细胞渗透性的 KIX-KID 相互作用的抑制剂。Naphthol AS-E 直接结合 CBP 的 KIX 域 (Kd: 8.6 µM)，阻断 KIX 域和 KID 域的相互作用 (IC50: 2.26 µM)。Naphthol AS-E 可用于癌症研究。
Cas No.92-78-4
别名色酚AS-E
Canonical SMILESO=C(C1=C(O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3
分子式C17H12ClNO2
分子量297.74
溶解度DMSO : 41.67 mg/mL (139.95 mM)
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

Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (Kd:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC50 of 2.26 µM. Naphthol AS-E can be used for cancer research.

CREB (cyclic AMP-response element-binding protein) is a downstream transcription factor of a multitude of signaling pathways emanating from receptor tyrosine kinases or G-protein coupled receptors.CREB can not be activated until it is phosphorylated at Ser133 and its subsequent binding to CREB-binding protein (CBP) through the kinase-inducible domain (KID) in CREB and KID-interacting (KIX) domain in CBP.In a cell-based CREB Renilla luciferase reporter assay, Naphthol AS-E inhibits CREB-mediated gene transcription with an IC50 of 2.29 µM. In HEK293T-based complementation assay, Naphthol AS-E dose-dependently inhibited Renilla luciferase activity with an IC50 of 2.9 µM by directly binding to CBP's KIX domain (Kd ~8.6 µM using a recombinant KIX).Naphthol AS-E exhibits low µM activity in inhibiting the proliferation of all these cancer cells, which is consistent with its cellular CREB inhibition potency. The average GI50 values for A549, MCF-7, MDA-MB-231 and MDA-MB-468 are approximately 2.9µM, 2.81µM, 2.35µM and 1.46µM, respectively.Naphthol AS-E (2.5 µM-10 µM; 48 hours) decreases the expression of anti-apoptotic protein Bcl-2. The expression of VEGF is also decreased.

References:
[1]. Fuchun Xie, et al. Synthesis and Evaluation of an O-Aminated Naphthol AS-E as a Prodrug of CREB-mediated Gene Transcription Inhibition. Lett Org Chem. 2013 Jun;10(5):380-384.
[2]. Bingbing X Li, et al. Discovery of a small-molecule inhibitor of the KIX-KID interaction. Chembiochem. 2009 Nov 23;10(17):2721-4.