Naphthol AS-E-武汉科斯坦生物科技有限公司

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Naphthol AS-E

英文名称：Naphthol AS-E

品牌：Chemstan

产地：中国

货号：CS-104068

cas：92-78-4

价格： ￥100/mg
发布日期： 2021-03-10
更新日期： 2025-12-31

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产地	中国
品牌	Chemstan
货号	CS-104068
用途	科研
包装规格	100 mg
纯度	98.00%%
CAS编号	92-78-4
别名
是否进口	否

Description

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 (K_d: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.

IC₅₀ & Target^[1]

KIX-KID

2.26 μM (IC₅₀)

In Vitro

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 (K_d ~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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

297.74

Formula

C??H??ClNO?

CAS No.

92-78-4

SMILES

O=C(C1=C(O)C=C2C=CC=CC2=C1)NC3=CC=C(Cl)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 41.67 mg/mL (139.95 mM; Need ultrasonic)

Preparing
Stock Solutions

ConcentrationSolventMass	1 mg	5 mg	10 mg

1 mM	3.3586 mL	16.7932 mL	33.5864 mL
5 mM	0.6717 mL	3.3586 mL	6.7173 mL
10 mM	0.3359 mL	1.6793 mL	3.3586 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: 2.5 mg/mL (8.40 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (8.40 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。

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.