生物活性分子抑制剂Pluripotin(Synonyms: SC1)

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。
Pluripotin (Synonyms: SC1) 纯度: 98.86%

Pluripotin 是 ERK1RasGAP 的双重抑制剂,KD 分别为 98 nM 和 212 nM。Pluripotin 还抑制 RSK1RSK2RSK3RSK4IC50 分别为 0.5,2.5,3.3 和 10.0 μM。

Pluripotin(Synonyms: SC1)

Pluripotin Chemical Structure

CAS No. : 839707-37-8

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Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1199 In-stock
2 mg ¥650 In-stock
5 mg ¥990 In-stock
10 mg ¥1750 In-stock
25 mg ¥3500 In-stock
50 mg ¥6200 In-stock
100 mg ¥8000 In-stock
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Pluripotin 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • MAPK Compound Library
  • Stem Cell Signaling Compound Library
  • Anti-Cancer Compound Library
  • Anti-Aging Compound Library
  • Reprogramming Compound Library
  • Oxygen Sensing Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Cancer Metabolism Compound Library
  • Anti-Obesity Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 µM, respectively.

IC50 & Target[1][2]

ERK1

98 nM (Kd)

RasGAP

212 nM (Kd)

RSK1

0.5 μM (IC50)

RSK2

2.5 μM (IC50)

RSK3

3.3 μM (IC50)

RSK4

10 μM (IC50)

体外研究
(In Vitro)

Pluripotin (SC-1) inhibits Abl1, p70S6K, PLK2, RSK1, RSK2, RSK3, RSK4 with IC50s of 0.005, 1.4, 2.2, 0.5, 2.5, 3.3, 10.0 µM,respectively. Pluripotin (SC-1) decreases cell growth for 7 colon tumor cell lines. After a five day exposure to 0.1 µM SC-1, the seven colon tumor lines are evaluated for changes in cell number and viability. There is a statistically significant decrease in cell number but >95% viability[2].

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

550.54

Formula

C27H25F3N8O2

CAS 号

839707-37-8

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 : ≥ 33 mg/mL (59.94 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8164 mL 9.0820 mL 18.1640 mL
5 mM 0.3633 mL 1.8164 mL 3.6328 mL
10 mM 0.1816 mL 0.9082 mL 1.8164 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 (4.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.54 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% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.54 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (4.54 mM) 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 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (4.54 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.54 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]. Chen S, et al. Self-renewal of embryonic stem cells by a small molecule. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17266-71.

    [2]. Mertins SD, et al. A small molecule (pluripotin) as a tool for studying cancer stem cell biology: proof of concept. PLoS One. 2013;8(2):e57099.

Cell Assay
[2]

The seven colon cancer lines (COLO 205, HCC-2998, HCT-15, HCT-116, HT29, KM12, SW-620) are used. In all experiments, each tumor line is cultured in 60 mm2 tissue culture treated dishes at an initial concentration of 62,500/mL (total 4 mL) before addition of 0.1 µM Pluripotin (SC-1) or an equivalent amount of diluent (DMSO) the next day. Five day exposures are conducted. The final concentration utilized for treatment for all tumor lines is determined by evaluating a range of SC-1 concentrations (0.01 to 10 µM) for sphere formation and any cytotoxic effects in the HCT-116 tumor line. Cell viability is routinely evaluated with the trypan blue exclusion test and is always >95% for concentrations at or below 0.1 µM[2].

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]. Chen S, et al. Self-renewal of embryonic stem cells by a small molecule. Proc Natl Acad Sci U S A. 2006 Nov 14;103(46):17266-71.

    [2]. Mertins SD, et al. A small molecule (pluripotin) as a tool for studying cancer stem cell biology: proof of concept. PLoS One. 2013;8(2):e57099.

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