HS38 is a potent, selective, and ATP-competitive inhibitor, targeting death-associated protein kinase 1 (DAPK1) and zipper-interacting protein kinase (ZIPK or DAPK3) with dissociation constants (Kds) of 300 nM and 280 nM, respectively. Additionally, it acts as a PIM3 inhibitor with an IC50 of 200 nM, showing potential for smooth muscle related disorder research[1].
体外研究
HS38 also shows a high affinity for DAPK2, with a Kd of 79 nM, although DAPK2 is not associated with smooth muscle contractility[1].
HS38 effectively decreases relative RLC20 phosphorylation in both basal and sphingosine 1-phosphate (S1P) activated states in human aortic smooth muscle (SM) cells and reduces contractile forces in intact mouse aorta and Ca2+-sensitized rabbit ileum tissue, indicating its impact on muscle relaxation and contractility[1].
HS38 细胞实验
Cell Line
Concentration
Treated Time
Description
References
human detrusor tissues
3 µM
30 minutes
To assess the effects of HS38 on carbachol-induced contractions. Results showed that HS38 did not affect contractions.
To assess the effects of HS38 on noradrenaline-, phenylephrine-, and methoxamine-induced contractions. Results showed that HS38 partially but inconsistently reduced contractions.
To assess the effects of HS38 on noradrenaline-, phenylephrine-, and methoxamine-induced contractions. Results showed that HS38 partially but inconsistently reduced contractions.
human coronary artery vascular smooth muscle cells (CASMCs)
50 μM
Evaluate the effect of HS38 on cofilin phosphorylation, results showed no significant effect of HS38 on cofilin phosphorylation
Sci Rep. 2016 Aug 30;6:32118
Coronary artery smooth muscle cells (CASMCs)
50 μM
16 hours
To investigate the effects of HS38 on the cytoskeletal architecture and FAK phosphorylation status of vascular smooth muscle cells. Results showed that HS38 treatment significantly altered F-actin cytoskeletal organization and reduced pY397-FAK phosphorylation levels.
Exp Physiol. 2023 Jul;108(7):986-997
HS38 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Sprague-Dawley rats
Posterior cerebral artery (PCA) vessel model
Ex vivo perfusion
10 μM
Single administration, lasting 30 minutes
To evaluate the inhibitory effect of HS38 on the myogenic response of posterior cerebral arteries. Results demonstrated that HS38 significantly attenuated vessel constrictions invoked by serotonin and intraluminal pressure elevation, and this dilatation was not associated with any change in myosin light chain (LC20) phosphorylation.
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