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BI-D1870
- Soluble in DMSO and EtOH
- MF: C19H23F2N5O2
- MW: 391.42
Description
Potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro (IC50 values 31 nM, 24 nM, 18 nM, and 15 nM, respectively).
* BI-D1870 binds at NTKD binding site as a reversible RSK inhibitor, while FMK (Axon 1848) binds at CTKD site as an irreversible RSK inhibitor.
More Information
| Parent CAS No. | 501437-28-1 |
|---|---|
| Chemical Name | 2-(3,5-Difluoro-4-hydroxy-phenylamino)-5,7-dimethyl-8-(3-methyl-butyl)-7,8-dihydro-5H-pteridin-6-one |
| SMILES | C1=NC(NC2C=C(F)C(O)=C(F)C=2)=NC2N(CCC(C)C)C(C)C(=O)N(C)C1=2 |
| MFCD | MFCD11223662 |
| InChi | InChI=1S/C19H23F2N5O2/c1-10(2)5-6-26-11(3)18(28)25(4)15-9-22-19(24-17(15)26)23-12-7-13(20)16(27)14(21)8-12/h7-11,27H,5-6H2,1-4H3,(H,22,23,24) |
| InChiKey | DTEKTGDVSARYDS-UHFFFAOYSA-N |
| CID | 25023738 |
| Short Description | RSK inhibitor |
References
- GP Sapkota et al. BI-D1870 is a specific inhibitor of the p90 RSK (ribosomal S6 kinase) isoforms in vitro and in vivo. Biochem. J. 2007, 401, 29–38.
- TL Nguyen. Targeting RSK: An Overview of Small Molecule Inhibitors. Anti-Cancer Agents Med. Chem. 2008, 8, 710-716.
- R Zaru et al. The MAPK-activated kinase Rsk controls an acute Toll-like receptor signaling response in dendritic cells and is activated through two distinct pathways. Nature Immunol. 2007, 8, 1227-1235.
- List of publications using BI-D1870 (Axon 1528) purchased from Axon Medchem
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