CTX-0294885 hydrochloride

CTX-0294885 hydrochloride is a sepharose-supported kinase capture reagent.

CTX-0294885 is a novel bisanilino pyrimidine exhibiting inhibitory activity against a broad range of kinases. CTx-0294885 represents a powerful new reagent for analysis of kinome signaling networks that may facilitate development of targeted therapeutic strategies. Large-scale CTx-0294885-based affinity purification followed by LC-MS/MS leads to the identification of 235 protein kinases from MDA-MB-231 cells, including all members of the AKT family that has not been previously detected by other broad-spectrum kinase inhibitors. Addition of CTx-0294885 to a mixture of three kinase inhibitors commonly used for kinase-enrichment increases the number of kinase identifications to 261. Combining CTx-0294885 with three other broad-specificity inhibitors for kinase enabled the identification of 799 highconfidence phosphosites on 183 kinases, 10% of which are localized to the activation loop, and included previously unreported phosphosites on BMP2K, MELK, HIPK2, and PRKDC[1].

[1]. Zhang L, et al. 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.