5.05300

RSK2 Inhibitor, RMM-46

• Synonym(s): RSK2 Inhibitor, RMM-46, ( E)-2-Cyano-N-(1-hydroxy-2-methylpropan-2-yl)-3-(3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl)acrylamide, RMM46, RSK Inhibitor IV, (E)-2-Cyano-N-(1-hydroxy-2-methylpropan-2-yl)-3-(3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl)acrylamide, RMM46, RSK Inhibitor IV
• Empirical Formula (Hill Notation): C₂₄H₂₆N₄O₅
• Molecular Weight: 450.49

Properties

• Ensaio: ≥98% (HPLC)
• Nível de qualidade: 100
• forma: solid
• manufacturer/tradename: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 50 mg/mL
• temperatura de armazenamento: 2-8°C

Description

Descrição geral

A cell-permeable cyanoacrylamide compound that acts as a potent, reversible, and selective inhibitor of ribosomal S6 kinase 2 (RSK2; IC₅₀ = 12 and 2.5 nM for wild-type and T493M RSK2, respectively). Shown to act by covalently modifying Cys436 at the ATP-binding site. Exhibits good selectivity over NEK2 and PLK1 (IC₅₀ = 530 nM and 2.2 µM) and does not affect the activity of a panel of 26 other protein kinases. Also shown to block phosphorylation of mitogen and stress activated kinases (MSK) 1, 2, and 3 in PMA-stimulated COS7 cells (IC₅₀ ~100 nM) and CREB phosphorylation in PMA- or UV-stimulated HeLa cells (IC₅₀ ~ 300 nM).

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
RSK2

Reversible: yes

Secondary Target
MSK 1, 2 , 3

Target IC₅₀: 12 and 2.5 nM for wild-type and T493M RSK2, respectively

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Reconstituição

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Use only fresh DMSO for reconstitution.

Outras notas

Miller, R.M., et al. 2013. J. Am. Chem. Soc.135, 5298.

Informações legais

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

Safety Information

• Código de classe de armazenamento: 11 - Combustible Solids
• WGK: WGK 2
• Ponto de fulgor (ºF): Not applicable
• Ponto de fulgor (ºC): Not applicable