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559286

Sigma-Aldrich

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.

Sinónimos:

RSK Inhibitor II, 2-(3,5-Difluoro-4-hydroxy-anilino)-8-isopentyl-5,7-dimethyl-7H-pteridin-6-one, racemic, p90 Ribosomal S6 Kinase Inhibitor II, BI-D1870, BID-1870, BID1870

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About This Item

Fórmula empírica (notación de Hill):
C19H23F2N5O2
Número de CAS:
Peso molecular:
391.42
Código UNSPSC:
12352200
NACRES:
NA.77

Nivel de calidad

Análisis

≥95% (HPLC)

formulario

solid

fabricante / nombre comercial

Calbiochem®

condiciones de almacenamiento

OK to freeze
protect from light

color

off-white

solubilidad

DMSO: 50 mg/mL

Condiciones de envío

ambient

temp. de almacenamiento

2-8°C

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)

Clave InChI

DTEKTGDVSARYDS-UHFFFAOYSA-N

Descripción general

The racemic mixture of a cell-permeable dihydropteridinone that acts as a potent and selective RSK inhibitor (IC50 ≤31 nM against RSK1, 2, 3, and 4; [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 HEK-293 cells and EGF-stimulated Rat-2 cells (IC50 ~1 µM).
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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Otras notas

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.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 2

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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François Sipieter et al.
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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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