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.

PKD:182 nM

在大鼠急性胰腺炎模型中,通过对PKD/ PKD1的抑制作用,CID755673可使坏死和胰腺炎的严重程度得到显著改善.

在HeLa细胞中,CID755673对PMA诱导的HDAC5核输出有显著阻断作用,且对PKD介导的蛋白质转运也有阻断作用。CID755673可直接抑制LNCaP前列腺癌细胞中PKD1的活性。CID755673有有效阻断前列腺癌细胞的迁移和侵入,并抑制肿瘤细胞增殖和细胞周期分布。

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)