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Key Documents

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.

Synonyme(s) :

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

Formule empirique (notation de Hill):
C19H23F2N5O2
Numéro CAS:
501437-28-1
Poids moléculaire :
391.42
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥95% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

off-white

Solubilité

DMSO: 50 mg/mL

Conditions d'expédition

ambient

Température de stockage

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)

Clé InChI

DTEKTGDVSARYDS-UHFFFAOYSA-N

Description générale

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.

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Autres remarques

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.

Informations légales

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

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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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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