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 inhibits S6K1 with an IC
50
of 0.8 μM.
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.
LJI308 (1-10 μM; 96 hours) decreases cell viability by up to 90%.
Cell Viability Assay
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Cell Line:
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HTRY-LT cell lines
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Concentration:
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1-10 μM
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Incubation Time:
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96 hours
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Result:
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Decreased cell viability by up to 90%.
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