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经验公式(希尔记法):
C19H23F2N5O2
化学文摘社编号:
分子量:
391.42
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
RSK Inhibitor II, The RSK Inhibitor II, also referenced under CAS 501437-28-1, controls the biological activity of RSK. This small molecule/inhibitor is primarily used for Cell Signaling applications.
SMILES string
Fc1c(c(cc(c1)Nc2nc3c(cn2)N(C(=O)C(N3CCC(C)C)C)C)F)O
InChI
1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24)
InChI key
DTEKTGDVSARYDS-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
off-white
solubility
DMSO: 50 mg/mL
shipped in
ambient
storage temp.
2-8°C
Quality Level
Disclaimer
Toxicity: Standard Handling (A)
General description
The racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 = 31, 24, 18, and 15 nM against RSK1, 2, 3, and 4, respectively; [ATP] = 100 µM) by targeting RSK N-terminal kinase domain in an ATP-competitive manner, while inhibiting 11 other kinases only at higher concentrations (IC50 ≥100 nM) and displaying little activity against 39 others. Shown to selectively inhibit RSK-dependent, but not RSK-independent, cellular protein phosphorylations in PMA-stimulated human HEK-293 cells and EGF-stimulated rat Rat-2 cells (IC50 ~1 µM). A useful pharmacological reagent for studying RSK-mediated cellular signaling events.
Other Notes
Carriere, A., et al. 2008. Curr. Biol.18, 1269
Sapkota, G.P., et al. 2007. Biochem. J.401, 29.
Zaru, R., et al. 2007. Nat. Immunol.8, 1227.
Sapkota, G.P., et al. 2007. Biochem. J.401, 29.
Zaru, R., et al. 2007. Nat. Immunol.8, 1227.
Packaging
Packaged under inert gas
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
François Sipieter et al.
iScience, 24(9), 103074-103074 (2021-09-28)
ERK1/2 involvement in cell death remains unclear, although many studies have demonstrated the importance of ERK1/2 dynamics in determining cellular responses. To untangle how ERK1/2 contributes to two cell death programs, we investigated ERK1/2 signaling dynamics during hFasL-induced apoptosis and
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