Thienopyridone

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Thienopyridone  纯度: 98.04%

Thienopyridone 是一种有效的选择性的肝再生磷酸酶 (PRL) 磷酸酶抑制剂，对于 PRL-1，PRL-2 和 PRL-3，IC50 值分别为 173 nM，277 nM 和 128 nM。Thienopyridone 对其他磷酸酶的影响很小。Thienopyridone 可诱导 p130Cas 裂解和细胞凋亡 (apoptosis)，并具有抗癌作用。

Thienopyridone

Thienopyridone Chemical Structure

CAS No. : 1018454-97-1

规格 价格 是否有货 数量
5 mg ￥3000 In-stock
10 mg ￥4800 In-stock
50 mg ￥13500 In-stock
100 mg ￥19500 In-stock
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500 mg   询价  

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Thienopyridone 相关产品

•相关化合物库:

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

生物活性

Thienopyridone is a potent and selective phosphatase of regenerating liver (PRL) phosphatase inhibitor with IC50s of 173 nM, 277 nM and 128 nM for PRL-1, PRL-2, and PRL-3, respectively. Thienopyridone shows minimal effects on other phosphatases. Thienopyridone induces p130Cas cleavage and apoptosis and has anticancer effects[1].

IC50 & Target

IC50: 173 nM (PRL-1), 277 nM (PRL-2) and 128 nM (PRL-3)[1]
体外研究
(In Vitro)

Thienopyridone shows significant inhibition of tumor cell anchorage-independent growth in soft agar. The EC50 values of the Thienopyridone are 3.29 μM and 3.05 μM for RKO and HT-29 cells, respectively[1].
Thienopyridone (1-75 μM; 24 hours; HeLa cells) treatment shows a dose-dependent down-regulation of total p130Cas in HeLa cells. Thienopyridone induces p130Cas and FAK cleavage leads to caspase-mediated cell apoptosis. Thienopyridone induces the cleavage of PARP and caspase-8[1].
Thienopyridone (3.75-30 μM; 24 hours) significantly suppresses HUVEC migration but not proliferation[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.

Cell Viability Assay[1]

Cell Line: RKO and HT-29 cells
Concentration: 0.5 μM, 1.67 μM, 5 μM, 8.33 μM
Incubation Time: 14 days
Result: Exhibited a dose-dependent inhibition in cancer cell anchorage-independent growth as measured by either colony number or colony size.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 1 μM, 5 μM, 10 μM, 25 μM, 50 μM, 75 μM
Incubation Time: 24 hours
Result: A dose-dependent down-regulation of total p130Cas was observed.

分子量

242.30

Formula

C13H10N2OS
CAS 号

1018454-97-1
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 : 5 mg/mL (20.64 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 80°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1271 mL 20.6356 mL 41.2712 mL
5 mM 0.8254 mL 4.1271 mL 8.2542 mL
10 mM 0.4127 mL 2.0636 mL 4.1271 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    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.58 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*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]. Daouti S, et al. A selective phosphatase of regenerating liver phosphatase inhibitor suppresses tumor cell anchorage-independent growth by a novel mechanism involving p130Cas cleavage. Cancer Res. 2008 Feb 15;68(4):1162-9.

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