LJI-308
产品编号: DC8812
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应用领域
LJI308是新型有效的RSK抑制剂, 抑制RSK1, RSK2, 和RSK3 IC50值分别为6 nM, 4 nM, 和13 nM。
| Cas No.: |
1627709-94-7 |
| 名称: |
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| 别名: |
LJI-308,LJI 308，LJI308 |
| SMILES: |
C(C1C=CC(N2CCOCC2)=CC=1)1C=CN=CC=1C1C=C(F)C(O)=C(F)C=1 |
| 分子式: |
C21H18F2N2O2 |
| 分子量: |
368.38 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| In Vitro: |
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| References: |
LJI308 is a selective and potent RSK inhibitor. Structural analysis confirms binding of LJH685 to the RSK2 N-terminal kinase ATP-binding site and reveals that the inhibitor adopts an unusual nonplanar conformation that explains its excellent selectivity for RSK family kinases. LJH685 and LJI308 efficiently inhibit RSK activity in vitro and in cells. Furthermore, cellular inhibition of RSK and its phosphorylation of YB1 on Ser102 correlate closely with inhibition of cell growth, but only in an anchorage-independent growth setting, and in a subset of examined cell lines. Thus, RSK inhibition reveals dynamic functional responses among the inhibitor-sensitive cell lines, underscoring the heterogeneous nature of RSK dependence in cancer. |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_2507_DC8812_1627709-94-7 |
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COA
| LOT NO. |
DOWNLOAD |
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