BMX-IN-1

Based on the data in Supplementary Table 1, this probe also binds to 63 other kinases (score less than or equal to 75%) at 1 micromolar concentration. So choosing a concentration well below 1 micromolar is critical for cell based studies. In addition, this probe is equipotent against BTK. BMX-IN-1 shows better selectivity than other known inhibitors of BMX, but even this probe can bind (and perhaps inhibit) a number of other kinases at higher concentrations.

BMX-IN-1 is an irreversible inhibitor of the kinase BMX and is the best available probe for it. It is also a potent inhibitor of BTK. In a broad kinome scan experiment (DiscoverX technology), BMX-IN-1 inhibits only 1% of the 442 kinases tested at >90% at a concentration of 1 micromolar. This is excellent selectivity. That said, there are potential off targets, so care should be taken in cell-based experiments to keep the dose as low as possible. The on-target, cell-based potency in a TEL-BMX transformed Ba/F3 cell line system is 25 nM. 1 micromolar of BMX-IN-1 inhibits autophosphorylation of BMX in RV-1 cells.