LJI308

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。

LJI308  纯度: 99.21%

LJI308 是一种有效的泛 RSK 抑制剂,对 RSK1、RSK2 和 RSK3 的 IC50 分别为 6 nM、4 nM 和 13 nM。LJI308 抑制辐照、EGF 处理和 表达 KRAS 突变的细胞中 RSK (T359/S363) 和 YB-1 (S102) 的磷酸化。

LJI308

LJI308 Chemical Structure

CAS No. : 1627709-94-7

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10 mM * 1 mL in DMSO ¥1216 In-stock
2 mg ¥990 In-stock
5 mg ¥1500 In-stock
10 mg ¥2500 In-stock
25 mg ¥5600 In-stock
50 mg ¥9900 In-stock
100 mg ¥16500 In-stock
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生物活性

LJI308 is a potent pan-ribosomal S6 kinase (RSK) inhibitor, with IC50s of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment with EGF, and in cells expressing a KRAS mutation[1][2].

体外研究
(In Vitro)

LJI308 inhibits S6K1 with an IC50 of 0.8 μM[1].
LJI308 inhibits YB-1 phosphorylation in CRC cells at concentrations of 5 to 25 μM. In a dose kinetics experiment, LJI308, starting at 2.5 μM, inhibits YB-1 phosphorylation in the KRAS mutated TNBC cell line MDA-MB-231 by approximately 86%. LJI308 effectively blocks RSK and YB-1 phosphorylation after EGF stimulation and after irradiation in KRAS wild-type HBL-100 cells[2].
LJI308 (1-10 μM; 96 hours) decreases cell viability by up to 90%[3].

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[3]

Cell Line: HTRY-LT cell lines
Concentration: 1-10 μM
Incubation Time: 96 hours
Result: Decreased cell viability by up to 90%.

分子量

368.38

Formula

C21H18F2N2O2

CAS 号

1627709-94-7

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 : 25 mg/mL (67.86 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7146 mL 13.5729 mL 27.1459 mL
5 mM 0.5429 mL 2.7146 mL 5.4292 mL
10 mM 0.2715 mL 1.3573 mL 2.7146 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% corn oil

    Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.79 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]. Aronchik I, et al. Novel potent and selective inhibitors of p90 ribosomal S6 kinase reveal the heterogeneity of RSK function in MAPK-driven cancers. Mol Cancer Res. 2014 May;12(5):803-12.

    [2]. Lettau K, et al. Simultaneous Targeting of RSK and AKT Efficiently Inhibits YB-1-Mediated Repair of Ionizing Radiation-Induced DNA Double-Strand Breaks in Breast Cancer Cells. Int J Radiat Oncol Biol Phys. 2021;109(2):567-580.

    [3]. Davies AH, et al. Inhibition of RSK with the novel small-molecule inhibitor LJI308 overcomes chemoresistance by eliminating cancer stem cells. Oncotarget. 2015;6(24):20570-20577.

    [4]. Jain R, et al. Discovery of Potent and Selective RSK Inhibitors as Biological Probes. J Med Chem. 2015 Sep 10;58(17):6766-83.

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