TM-04-176-01

Users are cautioned that selectivity data was collected at 1 µM so additional kinases may be inhibited when the compound is used above 1 µM.

The phosphatidylinositol 5-phosphate 4-kinases (PI5P4Ks) play critical roles in regulating numerous cell signalling pathways and thus are are considered attractive therapeutic targets in different human diseases such as cancer, immunological and neurodegenerative disorders. There are several pan-PI5P4Ks small-molecule inhibitors that have been reported (competitive or allosteric inhibition), including covalent inhibitors, which present different degrees of selectivity and/or potency in biochemical and/or cellular assays, or cell-permeability. In this context, among the selective pan-PI5P4Ks inhibitors, the reversible, ATP-site-directed inhibitor TM-04-176-01 posses the required characteristics to be a useful chemical probe, including an excellent potency and selectivity in both biochemical and cellular assays.

An orthogonal assay would be nice as in-cellular assay eg. dose-response assay. In-vitro potency insufficient. No cytotoxicity data is available. Very selective compound up to 1 µM.