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BI-D1870
- Soluble in DMSO and EtOH
- MF: C19H23F2N5O2
- MW: 391.42
Description
BI-D1870 is a highly potent and selective inhibitor of p90 ribosomal S6 kinase (RSK), targeting isoforms RSK1, RSK2, RSK3 and RSK4 with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM, respectively. Mechanistically, BI-D1870 acts as a reversible inhibitor at the N-terminal kinase domain (NTKD), whereas FMK (Axon 1848) irreversibly binds to the C-terminal kinase domain (CTKD).
RSK kinases act downstream of ERK/MAPK signaling to regulate transcription, translation, cell growth and survival. BI-D1870 is widely used to probe RSK-dependent signaling events and separate downstream RSK biology from upstream MEK/ERK activation.
Key Features
- Highly potent and selective pan-RSK inhibitor (RSK1-4)
- Targets a key downstream branch of ERK/MAPK signaling
- Useful for assessing RSK-dependent transcriptional and translational responses
- Cell-permeable tool for kinase signaling studies
Applications
- RSK kinase pharmacology
- MAPK downstream signaling research
- Cell proliferation and survival assays
- Kinase pathway selectivity studies
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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