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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 | |
|---|---|
| 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 | |
|---|---|
| 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.
| Related PKA Products |
|---|
| Bucladesine Sodium Salt
Bucladesine, a membrane permeable selective activator of PKA, has a critical role in up-regulation of ChAT and VAChT gene expression in PC12 cells by activation of extracellular signal regulated kinase (ERK) in Ca2+- and PKA-dependent manner. |
| H-89
H-89 is a potent PKA inhibitor with Ki of 48 nM, 10-fold selective for PKA than PKG, greater than 500-fold selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. |
| 8-Bromo-cAMP sodium salt
8-Bromo-cAMP is a cell perbeable cyclic AMP (cAMP) analog and a PKA activator. |
| 5-Iodotubercidin
5-IOdotubercidin (NSC 113939), an ATP analogue, is a potent inhibitor of adenosine kinase with an IC50 value of 26 nM. 5-IOdotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by activating phosphorylase and glycogen synthase. 5-IOdotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC, and Haspin inhibitors. |
| HA-100
Ha-100 is a potent protein kinase inhibitor with IC50 values of 4 μM, 8 μM, 12 μM and 240 μM against PKG, PKA, PKC and MLC kinases, respectively. Ha-100 is also used as a ROCK inhibitor. |
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