BAMB-4 is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay. Only BAMB-4 was nearly completely taken up by H1299 cells and remained stable after cellular uptake, thus exhibiting a robust stability and a high membrane permeability. Determination of the inhibitor type revealed that BAMB-4 belongs to the group of mixed type inhibitors. BAMB-4 is also a membrane-permeable InsP3Kinase inhibitor with IC50-value of 20 μM[2].
ITPKA inhibitor BAMB-4 exhibit the lowest inhibition frequency among the InsP3- Kinase inhibitors. Only in one from 42 targets tested, BAMB-4 showed an inhibitory effect. Noteworthy, in kinase screens no targets of BAMB-4 were detected, indicating that the compound does not belong to the typical kinase inhibitors. Thus, the relative high specificity and the high cellular uptake of BAMB-4 now for the test provide the possibility to effectively inhibit InsP3kinase in vivo. The InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancer therapy[3].
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