| Identification | Back Directory | [Name]
2-Propenamide, 2-cyano-N-(2-hydroxy-1,1-dimethylethyl)-3-[3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl]-, (2E)- | [CAS]
1627136-54-2 | [Synonyms]
RSK2-IN-3
2-Propenamide, 2-cyano-N-(2-hydroxy-1,1-dimethylethyl)-3-[3-(3,4,5-trimethoxyphenyl)-1H-indazol-5-yl]-, (2E)- | [Molecular Formula]
C24H26N4O5 | [MOL File]
1627136-54-2.mol | [Molecular Weight]
450.49 |
| Chemical Properties | Back Directory | [Boiling point ]
725.5±60.0 °C(Predicted) | [density ]
1.277±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 50mg/mL | [form ]
solid | [pka]
11.78±0.46(Predicted) | [color ]
yellow |
| Hazard Information | Back Directory | [Uses]
RSK2-IN-3 (Compound 26) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase[1]. | [Biological Activity]
Cell permeable: yes''Primary Target
RSK2''Reversible: yes''Secondary Target
MSK 12 3''Target IC50: 12 and 2.5 nM for wild-type and T493M RSK2respectively | [IC 50]
RSK2: 9.2 (pIC50, MSK1 CTKD); RSK2: 8.3 (pIC50, ERK2-MSK1 cascade) | [References]
[1] Hall A, et al. Discovery and Characterization of a Novel Series of Chloropyrimidines as Covalent Inhibitors of the Kinase MSK1. ACS Med Chem Lett. 2022 Jun 25;13(7):1099-1108. DOI:10.1021/acsmedchemlett.2c00134 |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|