CID755673
sodium (also known as benzoxoloazepinolone) is a novel, potent and selective
cell-active pan-PKD1/2/3 (Protein kinase D) inhibitor with IC50 of 180
nM, 280nM, and 227 nM, respectively, it shows about 200-fold selectivity
over other CAMKs. CID755673 is the first identified cell-active small
molecule PKD antagonist. It inhibits the activity of PKD1 with an IC50
of 182 nM and demonstrates highest selectivity to PKD1 when compared
with AKT, PLK1, CAK, CAMKIIα, PKD2 and PKD3. Moreover, it was not
competitive with ATP for enzyme inhibition. In HeLa cells, CID755673
significantly blocks PMA-induced nuclear export of HDAC5, and blocks
PKD-mediated protein transport.
纯度:≥98%