Molecular Formula | C18H19FN4O2 |
Molar Mass | 342.37 |
Density | 1.36 |
Storage Condition | -20℃ |
In vitro study | 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.921 ml | 14.604 ml | 29.208 ml |
5 mM | 0.584 ml | 2.921 ml | 5.842 ml |
10 mM | 0.292 ml | 1.46 ml | 2.921 ml |
5 mM | 0.058 ml | 0.292 ml | 0.584 ml |
biological activity | FMK is an irreversible RSK2 inhibitor that can covalently modify the C- terminal region of RSK. |
in vitro study | 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. |