HS-38 is a potent and selective DAPK1 and DAPK3 (ZIPK) inhibitor with IC50 of 200 nM for DAPK1 and Kd of 280 nM for ZIPK.
HS-38 also inhibits Pim3 (IC50=200 nM), and displays no activity against Src or Abl, little activity against EGFR.
HS-38 decreases RLC20 phosphorylation in cells, and decreases contractile force generated in mouse aorta, rabbit ileum, and calyculin A stimulated arterial muscle by decreasing RLC20 and MYPT1 phosphorylation.
HS-38 also promotes relaxation in Ca(2+)-sensitized vessels.
