CID755673 suppressed half of the PKD1 enzyme activity at 182 nm and exhibited selective PKD1 inhibition when compared with AKT, polo-like kinase 1 (PLK1), CDK activating kinase (CAK), CAMKIIalpha, and three different PKC isoforms.In cell-based assays, CID755673 blocked phorbol ester-induced endogenous PKD1 activation in LNCaP cells in a concentration-dependent manner. Functionally, CID755673 inhibited the known biological actions of PKD1 including phorbol ester-induced class IIa histone deacetylase 5 nuclear exclusion, vesicular stomatitis virus glycoprotein transport from the Golgi to the plasma membrane, and the ilimaquinone-induced Golgi fragmentation. Moreover, CID755673 inhibited prostate cancer cell proliferation, cell migration, and invasion. Treatment with CK59 and CID755673 indeed resulted in a significant dose-dependent reduction of NK cell degranulation markers and cytokine release in freshly isolated Peripheral blood mononuclear cell populations from healthy blood donors.
|Cell lines||LNCaP or PC3 cells|
|Preparation method||Counting the number of viable cells upon trypan blue staining to determine cell proliferation . Using cellTiter-Glo Luminescent Cell Viability Assay to measure Cell proliferation by according to the manufacturer's instructions.|
|Incubation time||6 days|
|Animal models||Rat pancreatitis model|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Protein Kinase Inhibitors CK59 and CID755673 Alter Primary Human NK Cell Effector Functions.
Scheiter M, et al. Front Immunol. 2013 Mar 18;4:66. PMID: 23508354.
Protein kinase D promotes in vitro osteoclast differentiation and fusion.
Mansky KC, et al. J Biol Chem. 2013 Apr 5;288(14):9826-34. PMID: 23430742.
CID755673 enhances mitogenic signaling by phorbol esters, bombesin and EGF through a protein kinase D-independent pathway.
Torres-Marquez E, et al. Biochem Biophys Res Commun. 2010 Jan 1;391(1):63-8. PMID: 19896460.
Potent and selective disruption of protein kinase D functionality by a benzoxoloazepinolone.
Sharlow ER, et al. J Biol Chem. 2008 Nov 28;283(48):33516-26. PMID: 18829454.
|Related PKD Products|
CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells.
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