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ATP-competitive inhibitor of DAPK (IC50 = 200 nM) and ZIPK (Kd = 280 nM). Also inhibits PIM3 kinase (IC50 = 200 nM) but exhibits no significant effect on Src or Abl kinases. Reduces phosphorylation of regulatory myosin light chain and myosin light chain phosphatase in mouse aortic and rabbit ileal tissues.

MacDonald et al (2016) A Small Molecule Pyrazolo[3,4-d]Pyrimidinone Inhibitor of Zipper-Interacting Protein Kinase Suppresses Calcium Sensitization of Vascular Smooth Muscle. Mol.Pharmacol. 89 105 PMID:26464323 |Carlson et al (2013) Fluorescence linked enzyme chemoproteomic strategy for discovery of a potent and selective DAPK1 and ZIPK inhibitor. ACS.Chem.Biol. 8 2715 PMID:24070067

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