产品
编 号:F469709
分子式:C18H19FN4O2
分子量:342.37
产品类型
结构图
CAS No: 821794-92-7
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产品详情
生物活性:
FMK is a an irreversible RSK2 kinase inhibitor, that covalently modifies the C-terminal kinase domain of RSK.
体外研究:
Pretreatment of ARVMs with 3 μM fmk attenuates the increase in Ser386 phosphorylation, but it has no inhibitory effect on the increase in Thr577 phosphorylation. FMK inhibits relatively few protein kinases in the panel, although it does inhibit protein tyrosine kinases, such as Src, Lck, Yes and Eph-A2, as well as S6K1. FMK will not inhibit RSK if the N-terminal kinase domain are activated by a mechanism that is independent of the C-terminal domain. Fmk potently inactivates the CTD auto-kinase activity of RSK1 and RSK2 with high specificity in mammalian cells. Targeting RSK2 by a specific small molecule RSK inhibitor fmk attenuates FGFR3-induced cytokine-independent growth in Ba/F3 cells. FMK inhibits cytokine-independent proliferation of Ba/F3 cells conferred by FGFR3.