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H-89 Dihydrochloride

Cat. No. M1729

All AbMole products are for research use only, cannot be used for human consumption.

H-89 Dihydrochloride Structure
Synonym:

H-89 2HCl

Size Price Availability Quantity
10mM*1mL in DMSO USD 49  USD49 In stock
5mg USD 36  USD36 In stock
10mg USD 55  USD55 In stock
25mg USD 110  USD110 In stock
50mg USD 219  USD219 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
References

[1] Lochner et al. Cardiovasc Drug Rev. The many faces of H89: a review.

[2] Davis MA, et al. J Pharmacol Exp Ther. Proteomic analysis of rat liver phosphoproteins after treatment with protein kinase inhibitor H89 (N-(2-[p-bromocinnamylamino-]ethyl)-5-isoquinolinesulfonamide).

[3] Geilen CC, et al. FEBS Lett. A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells.

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Keywords: H-89 Dihydrochloride, H-89 2HCl supplier, PKA, inhibitors, activators

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