Description:
FMK is a potent, highly specific and irreversible ribosomal s6 kinase (RSK) inhibitor that covalently modifies the C-terminal kinase domain of RSK. Its IC50 value is 15 nM. It could prevent the activation of the N-terminal kinase domain of RSK by the C-terminal kinase domain, but does not affect the activity of the N-terminal domain. It binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. It induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells. It is used to determine the role of RSK as a direct regulator of NHE1 phosphorylation and sarcolemmal NHE activity in this cell type, in response to 1-adrenergic stimulation.
- Molecular Weight:342.37
- Boiling Point:633.3±55.0 °C | Condition: Press: 760 Torr
- Purity:>98%
Molecular Formula:
C18H19FN4O2
Canonical SMILES:
CC1=CC=C(C=C1)C2=C(N(C3=C2C(=NC=N3)N)CCCO)C(=O)CF
InChI:
InChI=1S/C18H19FN4O2/c1-11-3-5-12(6-4-11)14-15-17(20)21-10-22-18(15)23(7-2-8-24)16(14)13(25)9-19/h3-6,10,24H,2,7-9H2,1H3,(H2,20,21,22)
InChIKey:
IKLGYJACVCXYIL-UHFFFAOYSA-N
Solubility:
10 mM in DMSO
Appearance:
White to off-white solid
Application:
FMK could prevent the activation of the N-terminal kinase domain of RSK by the C-terminal kinase domain, but does not affect the activity of the N-terminal domain. It is used to determine the role of RSK as a direct regulator of NHE1 phosphorylation and sarcolemmal NHE activity in this cell type, in response to 1-adrenergic stimulation.
Storage: -20°C Freezer
Synonyms:
1-[4-Amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoroethanone;RSK2 kinase inhibitor Más detalles se encuentran
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