In vitro activity: BAMB-4 (formerly known as ITPKA-IN-C14) is a novel and highly potent membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with IC50 of 37 uM in ADP-Glo Assay. Ectopic expression of the neuron-specific ITPKA in lung cancer cells increases their metastatic potential because the protein exhibits two actin regulating activities; it bundles actin filaments and regulates inositol-1,4,5-trisphosphate (InsP3)-mediated calcium signals by phosphorylating InsP3. Thus, in order to inhibit the metastasis-promoting activity of ITPKA, both its actin bundling and its InsP3kinase activity has to be blocked. 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.

Kinase Assay: BAMB-4 (formerly known as ITPKA-IN-C14) is a novel and highly potent membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase A (ITPKA) with IC50 of 37 uM in ADP-Glo Assay.

Cell Assay: