CID-2011756 is a novel and potent inhibitor of protein kinase D1 (PKD1), one of three PKD isoforms of a novel family of serine/threonine kinases involved in cell proliferation, survival, invasion and protein transport, with a value of 50% inhibition concentration IC50 of 3.2 μM in vitro. CID-2011756 also exhibits pan-PKD inhibitory effects that ATP-competitively inhibits PKD2 and PDK3 with values of IC50 of 0.6 μM and 0.7 μM respectively. Study results have shown that CID-2011756 is a cell active PKD1 inhibitor that concentration-dependently inhibits phorbolester-induced endogenous PKD1 activation in LNCap prostate cancer cells with a value of half maximal effective concentration EC50 of 10 μM.
Reference
[1].Sharlow ER, Mustata Wilson G, Close D, Leimgruber S, Tandon M, Reed RB, Shun TY, Wang QJ, Wipf P, Lazo JS. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.