STK16-IN-1

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STK16-IN-1  纯度: 99.49%

STK16-IN-1是STK16激酶抑制剂,IC50值为295 nM。

STK16-IN-1

STK16-IN-1 Chemical Structure

CAS No. : 1223001-53-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥847 In-stock
5 mg ¥770 In-stock
10 mg ¥1350 In-stock
25 mg ¥2850 In-stock
50 mg ¥5100 In-stock
100 mg ¥9100 In-stock
200 mg   询价  
500 mg   询价  

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STK16-IN-1 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Targeted Diversity Library

生物活性

STK16-IN-1 is a STK16 kinase inhibitor with an IC50 of 295 nM.

IC50 & Target

IC50: 295 nM (STK16)[1]

体外研究
(In Vitro)

STK16-IN-1, which exhibits potent inhibitory activity against STK16 kinase (IC50=0.295 μM) with excellent selective across the kinome as assessed using the KinomeScanTM profiling assay. STK16-IN-1 inhibits mTOR kinase with an IC50 of 5.56 μM. In MCF-7 cells, treatment with STK16-IN-1 results in a reduction in cell number and accumulation of binucleated cells, which can be recapitulated by RNAi knockdown of STK16. Co-treatment of STK16-IN-1 with chemotherapeutics such as cisplatin, doxorubicin, colchicine and paclitaxel results in a slight potentiation of the anti-proliferative effects of the chemotherapeutics. STK16-IN-1 provides a useful tool compound for further elucidating the biological functions of STK16)[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

293.30

Formula

C17H12FN3O

CAS 号

1223001-53-3

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 : 15 mg/mL (51.14 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4095 mL 17.0474 mL 34.0948 mL
5 mM 0.6819 mL 3.4095 mL 6.8190 mL
10 mM 0.3409 mL 1.7047 mL 3.4095 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 (8.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.52 mM,饱和度未知) 的澄清溶液。

    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;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: ≥ 2.5 mg/mL (8.52 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.52 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 25.0 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]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.

Kinase Assay
[1]

STK16-IN-1 is generally prepared with 1:3 serial dilutions for 4 concentrations (100 nM, 50 nM, 20 nM, and 10 nM); 6 concentrations are used (1 mM to 10 μM) for ATP competition experiments. The kinase reaction is performed with 1×kinase reaction buffer. Reactions in each well are started immediately by adding ATP and kept going for half an hour under 37°C. After the plate cooled for 5 minutes at room temperature, 5 μL of ADP-Glo reagent is added into each well to stop the reaction and consume the remaining ADP within 40 minutes. At the end, 10 μL of kinase detection reagent is added into the well and incubated for 1 hour to produce a luminescence signal[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 Assay
[1]

MCF-7, HCT116, HeLa cells are treated with STK16-IN-1 (0, 5, 10 μM) for 72 hours and apoptotic cells are analyzed by flow cytometry using Annexin V/PI apoptosis detection kit[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.

参考文献
  • [1]. Liu F, et al. Discovery of a Highly Selective STK16 Kinase Inhibitor. ACS Chem Biol. 2016 Jun 17;11(6):1537-43.

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