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
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About This Item
Empirical Formula (Hill Notation):
C24H26N4O5
CAS Number:
Molecular Weight:
450.49
UNSPSC Code:
12352200
assay
≥98% (HPLC)
Quality Segment
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 50 mg/mL
storage temp.
2-8°C
General description
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
RSK2
Reversible: yes
Secondary Target
MSK 1, 2 , 3
MSK 1, 2 , 3
Target IC50: 12 and 2.5 nM for wild-type and T493M RSK2, respectively
Packaging
Packaged under inert gas
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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