Uses
BPKDi is a potent bipyridyl PKD inhibitor with IC50s of 1 nM, 9 nM and 1 nM for PKD1, PKD2 and PKD3, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes[1].
Biological Activity
BPKDi is an inhibitor of protein kinase D (PKD; IC50s = 1, 9, and 1 nM for PKD1, PKD2, and PKD3, respectively).1 It is selective for PKD over PKCδ and PKCε, as well as over a panel of additional calcium/calmodulin-dependent protein kinase (CaMK) superfamily members, at 1 μM. It inhibits phenylephrine-induced phosphorylation and nuclear export of histone deacetylase 4 (HDAC4) and HDAC5 in, as well reduces phenylephrine-induced hypertrophy of, isolated neonatal rat ventricular myocytes when used at a concentration of 1 μM.
IC 50
PKD1: 1 nM (IC50); PKD2: 9 nM (IC50); PKD3: 1 nM (IC50)
References
1.Monovich, L., Vega, R.B., Meredith, E., et al.A novel kinase inhibitor establishes a predominant role for protein kinase D as a cardiac class IIa histone deacetylase kinaseFEBS Lett.584(3)631-637(2010)
