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H-89 dihydrochloride is an inhibitor of PKA and MSK, inhibits cyclic-AMP response element binding protein-mediated MAPK phosphatase-1 induction by lipopolysaccharide. The Ki value is 48 nM for PKA inhibitor. H-89 having a relatively large number of PKA-independent effects which may seriously compromise interpretation of data, and it also inhibits at least 8 other kinases. H-89 significantly inhibits the forskolin-induced neurite outgrowth from PC12D cells.
H-89 (30 μM) inhibits significantly cAMP-dependent histone IIb phosphorylation activity in PC12D cell lysates. H-89 (1-2 μM) significantly slows the repriming rate in rat skinned fibres, most likely due to it deleteriously affecting the T-system potential.
H-89 (0.2 mg/100g, i.p.) significantly increases seizure latency and threshold in PTZ-treated animals. H-89 (0.05, 0.2 mg/100 g, i.p.) prevents the epileptogenic activity of bucladesine (300 nM) with significant increase of seizure latency and seizure threshold.
Cell Experiment | |
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Cell lines | Hela cells |
Preparation method | Choline uptake. Choline uptake was measured as described.Briefly. cells grown on colleen-coated plastic sheets, were preincubated for 30 min with medium containing H-89 or no supplements ascontrol, After preincubation, cells were immersed in medium with or without H-89, containing choline(5μCi/ml), After different times, cells were washed throughly with 58mmol/l choline chloride in PBS. Finally, uptake and incorpration of [H] choline were determined by liquid scintillation counting. background radioactivity was measured by repeating the experiment at 4℃. |
Concentrations | 0~100μM |
Incubation time | 1 h |
Animal Experiment | |
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Animal models | Adult male Sprague-Dawley rats model |
Formulation | 5% DMSO in 0.9% sterile saline |
Dosages | 20 mg/kg or 200mg/kg twice daily |
Administration | oral gavage |
Molecular Weight | 519.28 |
Formula | C20H20BrN3O2S.2HCl |
CAS Number | 130964-39-5 |
Solubility (25°C) | DMSO 60 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Lochner et al. Cardiovasc Drug Rev. The many faces of H89: a review.
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