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RSK Inhibitor II

Name: RSK Inhibitor II
Brand: MM

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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Fórmula empírica (notación de Hill):

C₁₉H₂₃F₂N₅O₂

Número CAS:

501437-28-1

Peso molecular:

391.42

MDL number:

MFCD11223662

UNSPSC Code:

12352200

NACRES:

NA.77

Assay:

≥95% (HPLC)

Form:

solid

Storage condition:

OK to freeze, protect from light

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Propiedades

Quality Segment

100

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

Descripción

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.

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c