CID755673 is an effective and specific cell-active inhibitor for PKD (IC50: 182 nM); exhibits selective PKD1 inhibition when compared with PLK1, AKT, CAMKIIα, CAK, and PKC isoforms.

PKD3:227 nM, PKD:182 nM, PKD2:280 nM

In an acute pancreatitis model in rats, CID755673 significantly ameliorates the severity of necrosis and pancreatitis through its inhibitory action on PKD/PKD1.

In HeLa cells, CID755673 significantly blocks the PMA-induced nuclear export of HDAC5 and also inhibits protein transport mediated by PKD. Furthermore, CID755673 directly inhibits the activity of PKD1 in LNCaP prostate cancer cells. This compound effectively prevents the migration and invasion of prostate cancer cells, as well as inhibiting tumor cell proliferation, and altering cell cycle distribution.

In Vitro Radiometric PKD Kinase Assay: The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.

Cell proliferation was determined by counting the number of viable cells upon trypan blue staining. Cell proliferation is measured by CellTiter-Glo Luminescent Cell Viability Assay according to the manufacturer's instructions.(Only for Reference)