标签归档：eya

NCGC00249987

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

NCGC00249987  纯度: 99.86%

NCGC00249987 是一种高度选择性和变构 Eya2 的 Tyr 磷酸酶活性的抑制剂，对 Eya2 ED 和 MBP-Eya2 FL 的 IC50 分别为 3 μM 和 6.9 μM。NCGC00249987 专门针对肺癌细胞的迁移，侵袭伪足形成和侵袭。

NCGC00249987

NCGC00249987 Chemical Structure

CAS No. : 1384864-80-5

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5 mg ￥1500 In-stock
10 mg ￥2500 In-stock
25 mg ￥4500 In-stock
50 mg ￥7500 In-stock
100 mg ￥12000 In-stock
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NCGC00249987 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

生物活性

NCGC00249987 is a highly selective and allosteric Tyr phosphatase activity of Eya2 inhibitor with IC50s of 3 μM and 6.9 μM for Eya2 ED and MBP-Eya2 FL. NCGC00249987 specifically targets migration, invadopodia formation, and invasion of lung cancer cells[1].

IC50 & Target

IC50: 3 μM (Eya2 ED) and 6.9 μM (MBP-Eya2 FL)[1]
体外研究
(In Vitro)

NCGC00249987 inhibits Eya2 ED (C-terminal Eya Domain). NCGC00249987 inhibits full length Eya2 including but not other Eya family members[1].
NCGC00249987 binding leads to a conformational change of the active site that is unfavorable for Mg2+ binding, thereby inhibiting Eya2’s Tyr phosphatase activity[1].
NCGC00249987 (5, 10 μM) treatment effectively suppresses migration, invadopodia formation and invasion in Eya2 WT expressing Calu-6 cells, but not in EV Calu-6 cells. NCGC00249987 does not inhibit cell growth or survival[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

342.35

Formula

C16H11FN4O2S
CAS 号

1384864-80-5
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)
参考文献

  • [1]. Anantharajan J, et al. Structural and Functional Analyses of an Allosteric EYA2 Phosphatase Inhibitor That Has On-Target Effects in Human Lung Cancer Cells. Mol Cancer Ther. 2019 Sep;18(9):1484-1496.

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MLS000544460

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MLS000544460  纯度: 99.74%

MLS000544460 是一种高度选择性和可逆的 Eya2 磷酸酶抑制剂，Kd 为 2.0 μM，IC50 为 4 μM。MLS000544460 抑制 Eya2 磷酸酶介导的细胞迁移，并具有抗癌活性。

MLS000544460

MLS000544460 Chemical Structure

CAS No. : 352336-36-8

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥2500 In-stock
10 mg ￥4500 In-stock
25 mg ￥8500 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

MLS000544460 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Metabolism/Protease Compound Library
  • Anti-Cancer Compound Library
  • Phosphatase Inhibitor Library
  • Targeted Diversity Library

生物活性

MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity[1].

IC50 & Target

Kd: 2.0 μM (Eya2 phosphatase)[1]
IC50: 4 μM (Eya2 phosphatase)[1]
体外研究
(In Vitro)

MLS000544460 does not bind Eya3 phosphatase (ED)[1].
MLS000544460 (10 μM) inhibits Eya2-mediated cell migration in human Eya2, Eya2 phosphatase-dead (D274N), and YFP (as a negative control) expressing MCF10A cells[1].
When Eya2 ED is dialyzed into 10 μM EDTA to remove Mg2+, it binds MLS000544460 with a higher affinity (Kd=0.80 μM), indicating that this class of compounds does not require Mg2+ for its interaction with the Eya2 ED[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

341.36

Formula

C17H12FN3O2S
CAS 号

352336-36-8
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL (366.18 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9295 mL 14.6473 mL 29.2946 mL
5 mM 0.5859 mL 2.9295 mL 5.8589 mL
10 mM 0.2929 mL 1.4647 mL 2.9295 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: ≥ 2.08 mg/mL (6.09 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.09 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.09 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Krueger AB, et al. Allosteric inhibitors of the Eya2 phosphatase are selective and inhibit Eya2-mediated cellmigration. J Biol Chem. 2014 Jun 6;289(23):16349-61.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务