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).
Biochem/physiol Actions
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
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
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.
Other Notes
Miller, R.M., et al. 2013. J. Am. Chem. Soc.135, 5298.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class
11 - Combustible Solids
wgk_germany
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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