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C19H23F2N5O2
CASçªå·:
ååé:
391.42
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
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ãæäŒãããŸãQuality Segment
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
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
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 â¥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.
Packaging
Packaged under inert gas
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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11 - Combustible Solids
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WGK 2
åŒç«ç¹ (F)
Not applicable
åŒç«ç¹ïŒÂ°CïŒ
Not applicable
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