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。
生物活性 | LJI308 is a potent pan-ribosomal S6 kinase (RSK)inhibitor, withIC50s of 6 nM, 4 nM, and 13 nM forRSK1,RSK2, andRSK3, respectively. LJI308 inhibits the phosphorylation of RSK (T359/S363) and YB-1 (S102) after irradiation, treatment withEGF, and in cells expressing a KRAS mutation[1][2]. |
体外研究 (In Vitro) | LJI308 inhibits S6K1 with an IC50of 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].
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%. |
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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 |
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溶解性数据 | In Vitro: DMSO : 25 mg/mL(67.86 mM;Need ultrasonic) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 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。
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