RSK2 Inhibitor, RMM-46

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

Toxicity: Standard Handling (A)

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).

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

Packaged under inert gas

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.

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