中文同义词:
RSK2抑制剂(FMK);1-[4-氨基-7-(3-羟基丙基)-5-(4-甲基苯基)-7H-吡咯并[2,3-D]嘧啶-6-基]-2-氟乙酮
英文名称:
1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone
英文同义词:
FMK;1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone;FMK - RSK inhibitor Fmk;1-(4-Amino-7-(3-hydroxypropyl)-5-(p-tolyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)-2-fluoroethanone;RSK2 kinase inhibitor;Ethanone, 1-[4-amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoro-;1-[5-amino-9-(3-hydroxypropyl)-7-(4-methylphenyl)-2,4,9-triazabicyclo[4.3.0]nona-1,3,5,7-tetraen-8-yl]-2-fluoro-ethanone
相关类别:
细胞生物学试剂;Akt;mTOR;PI3K;API
生物活性
FMK 是一种不可逆的 RSK2 抑制剂，能够共价修饰 RSK 的 C 末端区域。
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.
