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H-89 Dihydrochloride

Cat. No. M1729
H-89 Dihydrochloride Structure
Synonym:

H-89 2HCl

Size Price Availability Quantity
10mg USD 80 In stock
50mg USD 260 In stock
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Quality Control
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. 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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 519.28
Formula C20H20BrN3O2S.2HCl
CAS Number 130964-39-5
Purity 100.00%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

The many faces of H89: a review.
Lochner et al. Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):261-74. PMID: 17214602.

Proteomic analysis of rat liver phosphoproteins after treatment with protein kinase inhibitor H89 (N-(2-[p-bromocinnamylamino-]ethyl)-5-isoquinolinesulfonamide).
Davis MA, et al. J Pharmacol Exp Ther. 2006 Aug;318(2):589-95. PMID: 16687476.

A selective inhibitor of cyclic AMP-dependent protein kinase, N-[2-bromocinnamyl(amino)ethyl]-5-isoquinolinesulfonamide (H-89), inhibits phosphatidylcholine biosynthesis in HeLa cells.
Geilen CC, et al. FEBS Lett. 1992 Sep 14;309(3):381-4. PMID: 1516714.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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