cct007093 is a small-molecule chemical inhibitor of ppm1d with ic50 value of 8.4μm [1].cct007093 is a thienylidene cyclopentanone and shows a potent inhibition of ppm1d in the in vitro assay when using the recombinant phospho-p38 as a substrate. in cellular assay, cct007093 shows specificity for mcf-7 cells over hela cells. it reduces 40% viability of the cells after 2 days. it is found that the cell death induced by cct007093 is dependent on p38 kinase activity. cct007093 mimics the effect of ppm1d rnai in activating p38 kinase. it induces p38 phosphorylation at 4 h post-exposure in mcf-7 cells and the loss of viability can be rescued by sb203580, the specific p38 inhibitor [1].
[1] rayter s, elliott r, travers j, rowlands mg, richardson tb, boxall k, jones k, linardopoulos s, workman p, aherne w, lord cj, ashworth a. a chemical inhibitor of ppm1d that selectively kills cells overexpressing ppm1d. oncogene. 2008 feb 14;27(8):1036-44.
