| Bioactivity | HS38 is a potent, selective, and ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK, also called DAPK3), with Kds of 300 nM and 280 nM, respectively. HS38 is also a PIM3 inhibitor with an IC50 of 200 nM. HS38 can be used for the research of smooth muscle related disorders[1]. | ||||||||||||
| Target | Kd: 300 nM (DAPK1), 79 nM (DAPK2), 280 nM (ZIPK), IC50: 200 nM (DAPK1), 200 nM (PIM3) | ||||||||||||
| Invitro | HS38 displays high affinity toward DAPK2, with a Kd of 79 nM. DAPK2 is not implicated in smooth muscle contractility[1].HS38 significantly reduces relative RLC20 phosphorylation in both the basal and sphingosine 1-phosphate (S1P) activated states in human aortic SM cells[1].HS38 reduces contractile forces generated by intact mouse aorta in aortic tissue[1].HS38 reduces the contractile force, RLC20 phosphorylation, and MYPT1 phosphorylation in Ca2+-sensitized rabbit ileum[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
| Name | HS38 | ||||||||||||
| CAS | 1030203-81-6 | ||||||||||||
| Formula | C14H12ClN5O2S | ||||||||||||
| Molar Mass | 349.80 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. David A Carlson, et al. Fluorescence Linked Enzyme Chemoproteomic Strategy for Discovery of a Potent and Selective DAPK1 and ZIPK Inhibitor. ACS Chem Biol. 2013 Dec 20; 8(12): 2715–2723. |