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. It has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor.Protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively). Cell permeable (EC50 = 10 μM for PKD1 inhibition).
|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.
Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity.
Sharlow ER, et al. PLoS One. 2011;6(10):e25134. PMID: 21998636.
|Related PKD Products|
CID755673 is a potent and selective cell-active small molecule inhibitor for PKD with an IC50 of 182 nM.
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