LJH-685

产品编号: DC8811 Featured
LJH-685
结构式
1627710-50-2
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中国地区超过5000个高品质化合物库存
应用领域
LJH685 是一种有效的选择性 RSK 抑制剂, 抑制 RSK1/2/3 生物活性, IC50 为 6、5、4 nM。
Cas No.: 1627710-50-2
名称:
别名: LJH-685,LJH 685,LJH685
SMILES: C1(=C(C2=CC(F)=C(O)C(F)=C2)C=NC=C1)C1=CC=C(N2CCN(C)CC2)C=C1
分子式: C22H21F2N3O
分子量: 381.42
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: LJH685 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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