CTX-0294885

Description: CTX-0294885 is a novel potent and broad-spectrum kinase inhibitor and a sepharose-supported kinase capture reagent which exhibits inhibitory activity against a broad range of kinases in vitro. Use of a quantitative proteomics approach confirmed the selectivity of CTx - 0294885 -bound beads for kinase enrichment. Large-scale CTX- 0294885 -based affinity purification followed by LC-MS/MS led to the identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that had not been previously detected by other broad-spectrum kinase inhibitors. CTX- 0294885 represents a powerful new reagent for analysis of kinome signaling networks that may facilitate development of targeted therapeutic strategies.

References: Zhang L, Holmes IP, Hochgräfe F, Walker SR, Ali NA, Humphrey ES, Wu J, de Silva M, Kersten WJ, Connor T, Falk H, Allan L, Street IP, Bentley JD, Pilling PA, Monahan BJ, Peat TS, Daly RJ. Characterization of the novel broad-spectrum kinase inhibitor CTx-0294885 as an affinity reagent for mass spectrometry-based kinome profiling. J Proteome Res. 2013 Jul 5; 12(7):3104-16. doi: 10.1021/pr3008495. Epub 2013 Jun 25. PubMed PMID: 23692254.