2. Epigenetics
  3. Histone Acetyltransferase Epigenetic Reader Domain
  4. Naphthol AS-E

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。

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Naphthol AS-E Chemical Structure

Naphthol AS-E Chemical Structure

CAS No. : 92-78-4

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10 mM * 1 mL in DMSO ￥660
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Customer Review

Naphthol AS-E 相关抗体

Top Publications Citing Use of Products

查看 Histone Acetyltransferase 亚型特异性产品:

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CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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.

IC50 & Target[1]

KIX-KID

2.26 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
2.9 μM
Compound: 1
Growth inhibition of human A549 cells after 72 hrs by MTT assay
Growth inhibition of human A549 cells after 72 hrs by MTT assay
[PMID: 25313320]
A549 GI50
2.9 μM
Compound: 1a
Growth inhibition of human A549 cells after 72 hrs by MTT assay
Growth inhibition of human A549 cells after 72 hrs by MTT assay
[PMID: 23102993]
HEK-293T IC50
2.29 μM
Compound: 1
Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as reduction in CREB-mediated gene tanscription after 5 hrs by luciferase reporter gene assay
Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as reduction in CREB-mediated gene tanscription after 5 hrs by luciferase reporter gene assay
[PMID: 25313320]
HEK-293T IC50
2.29 μM
Compound: 1a
Inhibition of CREB-mediated gene transcription in human HEK293T cells by renilla luciferase reporter assay
Inhibition of CREB-mediated gene transcription in human HEK293T cells by renilla luciferase reporter assay
[PMID: 23102993]
HEK-293T IC50
2.29 μM
Compound: Naphthol AS-E, 1
Inhibition of CREB expressed in HEK293T cells assessed as inhibition of forskolin-stimulated CRE transcription incubated for 30 mins prior to forskolin-stimulation measured after 4.5 hrs by luciferase reporter gene assay
Inhibition of CREB expressed in HEK293T cells assessed as inhibition of forskolin-stimulated CRE transcription incubated for 30 mins prior to forskolin-stimulation measured after 4.5 hrs by luciferase reporter gene assay
[PMID: 22458559]
MCF7 GI50
2.81 μM
Compound: 1
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
[PMID: 25313320]
MCF7 GI50
2.81 μM
Compound: 1a
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
Growth inhibition of human MCF7 cells after 72 hrs by MTT assay
[PMID: 23102993]
MDA-MB-231 GI50
2.35 μM
Compound: 1
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 25313320]
MDA-MB-231 GI50
2.35 μM
Compound: 1a
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-231 cells after 72 hrs by MTT assay
[PMID: 23102993]
MDA-MB-468 GI50
1.46 μM
Compound: 1
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
[PMID: 25313320]
MDA-MB-468 GI50
1.46 μM
Compound: 1a
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
Growth inhibition of human MDA-MB-468 cells after 72 hrs by MTT assay
[PMID: 23102993]
体外研究
(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 (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.

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

Naphthol AS-E 相关抗体:
分子量

297.74

Formula

C17H12ClNO2
CAS 号
性状

固体

颜色

Light brown to brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 41.67 mg/mL (139.95 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

    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); 悬浊液; 超声助溶

    此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (8.40 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

Naphthol AS-E 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3586 mL 16.7932 mL 33.5864 mL 83.9659 mL
5 mM 0.6717 mL 3.3586 mL 6.7173 mL 16.7932 mL
10 mM 0.3359 mL 1.6793 mL 3.3586 mL 8.3966 mL
15 mM 0.2239 mL 1.1195 mL 2.2391 mL 5.5977 mL
20 mM 0.1679 mL 0.8397 mL 1.6793 mL 4.1983 mL
25 mM 0.1343 mL 0.6717 mL 1.3435 mL 3.3586 mL
30 mM 0.1120 mL 0.5598 mL 1.1195 mL 2.7989 mL
40 mM 0.0840 mL 0.4198 mL 0.8397 mL 2.0991 mL
50 mM 0.0672 mL 0.3359 mL 0.6717 mL 1.6793 mL
60 mM 0.0560 mL 0.2799 mL 0.5598 mL 1.3994 mL
80 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0496 mL
100 mM 0.0336 mL 0.1679 mL 0.3359 mL 0.8397 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Naphthol AS-E92-78-4Histone AcetyltransferaseEpigenetic Reader DomainHATsHATKIX-KIDA549MCF-7MDA-MB-231cancerCBPCREBInhibitorinhibitorinhibit

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