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. As we recognized its kinase inhibiting properties, H89 should not be used as the single source of evidence of PKA involvement, it should be used in conjunction with other PKA inhibitors, such as Rp-cAMPS or PKA analogs.
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 54 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Lochner et al. Cardiovasc Drug Rev. The many faces of H89: a review.
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