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    H 89 2HCl
    H 89 2HCl

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0243
    CAS #: 130964-39-5Purity ≥98%

    Description: H 89 2HCl, the dihydrochloride salt of H 89 (H-89), is a novel, potent and cAMP-dependent inhibitor of PKA (protein kinase A) with the potential to attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice. It inhibits PKA with a Ki of 48 nM in a cell-free assay, shows 10-fold selectivity for PKA over PKG, and exhibits 500-fold higher selectivity than PKC, MLCK, calmodulin kinase II and casein kinase I/II. 

    References:J Biol Chem. 1990 Mar 25;265(9):5267-72; Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):261-74.

    Related CAS #: 127243-85-0 (free base); 1000995-75-4 (free base); 1049740-55-7 (2HCl hydrate)    

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    • 香港大学
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    Molecular Weight (MW)

    519.28

    Formula

    C20H20BrN3O2S.2HCl

    CAS No.

    130964-39-5

    Storage

    -20℃ for 3 years in powder form

    -80℃ for 2 years in solvent

    Solubility (In vitro)

    DMSO: 104 mg/mL (200.3 mM)

    Water: 6 mg/mL (11.6 mM)

    Ethanol:  <1 mg/mL

    Solubility (In vivo)

    1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL

    Synonyms

    Synonym: H-89; H-89 Dihydrochloride; H89; H 89 HCl.

    Chemical Name: N-[2-[[3-(4-Bromophenyl)-2-propen-1-yl]amino]ethyl]-5-Isoquinolinesulfonamide dihydrochloride

    InChi Key: GELOGQJVGPIKAM-WTVBWJGASA-N

    InChi Code: InChI=1S/C20H20BrN3O2S.2ClH/c21-18-8-6-16(7-9-18)3-2-11-22-13-14-24-27(25,26)20-5-1-4-17-15-23-12-10-19(17)20;;/h1-10,12,15,22,24H,11,13-14H2;2*1H/b3-2+;;

    SMILES Code: O=S(C1=CC=CC2=C1C=CN=C2)(NCCNC/C=C/C3=CC=C(Br)C=C3)=O.[H]Cl.[H]Cl


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    In Vitro

    In vitro activity: H89 2HCl is a potent PKA (cAMP-dependent) protein kinase A inhibitor with Ki of 48 nM, exhibits 10-fold selectivity over PKG, exhibits >500-fold selectivity over PKC, MLCK, calmodulin kinase II and casein kinase I/II. Pretreatment of the cells with H-89 (30 μM) 1 h before the addition of forskolin markedly inhibits the forskolin-induced protein phosphorylation in a dose-dependent manner. H89 also inhibits several other kinases with IC50 of 80, 120, 135, 270, 2600 and 2800 nM for S6K1, MSK1, PKA, ROCKII, PKBα and MAPKAP-K1b, respectively. H89 also has activity at some cellular receptors and ion channels, including Kv1.3 K+ channels,β1AR and β2AR.

     

    Kinase Assay: PKA enzyme activity: cAMP-dependent protein kinase activity is assayed in a reaction mixture containing, in a final volume of 0.2 mL, 50 mM Tris-HC1 (pH 7.0), 10 mM magnesium acetate, 2 mM EGTA, 1 μM cAMP or absence of cAMP, 3.3-20 μM [γ-32P]ATP (4 × 105 cpm), 0.5 μg of the enzyme, 100 μg of histone H2B, and each compound, as indicated.

     

    Cell Assay: Levels of intracellular cAMP are determined. After 48 h in culture, PC12D cells are cultured in test medium containing 30 μM H-89 for 1 h and then exposed to fresh medium that contained both 10 μM forskolin and 30 μM H-89. Cells are scraped off with a rubber policeman and sonicated in the presence of 0.5 ml of 6% trichloroacetic acid. To extract trichloroacetic acid, 2 ml of petroleum ether is added, the preparation mixed and centrifuged at 3000 rpm for 10 min. After aspiration of the upper layer, the residue sample solution is used for determination.

    In Vivo

    H89 causes distinct modifications of protein phosphorylation, with the most robust changes in phosphorylation are fructose-1,6-biphosphatase, heterogeneous nuclear ribonucleoprotein (hnRNP), NSFL1 cofactor p47, all which have potentially regulatory connections to cAMP/PKA. H-89 (0.5, 1, 5 mg/kg) significantly attenuates prominent behavioral signs of morphine withdrawal in morphine-dependent mice.

    Animal model

    Mouse and rat

    Formulation & Dosage

    Dissolved in 100% DMSO, diluted 1:20 in 0.9% sterile saline (Rat); 1% DMSO (Mice); 20 or 200 mg/kg (Rat); 0-5 mg/kg (Mice); s.c. (rat); i.p. (mice)

    References

    J Biol Chem. 1990 Mar 25;265(9):5267-72; Cardiovasc Drug Rev. 2006 Fall-Winter;24(3-4):261-74; J Pharmacol Exp Ther. 2006 Aug;318(2):589-95; Sci Signal. 2008 Jun 3;1(22):re4.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    H 89 2HCl


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