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    KN-62
    KN-62

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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 #: V1298
    CAS #: 127191-97-3Purity ≥98%

    Description: KN-62 (KN62; KN 62) is a potent, selective, cell-permeable and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with potential anticancer activity. It inhibits CaMKII with a Ki of 0.9 μM. KN62 inhibits the invasiveness of cancer cells in vitro and in vivo KN62 causes retrograde amnesia in the rat. KN62 attenuates glutamate release by inhibiting voltage-dependent Ca2+-channels. The effect of KN62 on Ca2+-influx appears to be specific to slowly-or non-inactivating conductances, and therefore presents KN62 as a potentially useful tool.  

    References: J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87.

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    Molecular Weight (MW)721.84
    FormulaC38H35N5O6S2
    CAS No.127191-97-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (138.5 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (S)-4-(2-(N-methylisoquinoline-5-sulfonamido)-3-oxo-3-(4-phenylpiperazin-1-yl)propyl)phenyl isoquinoline-5-sulfonate

    SMILES Code: CN([[email protected]@H](CC1=CC=C(OS(=O)(C2=C3C(C=NC=C3)=CC=C2)=O)C=C1)C(N4CCN(C5=CC=CC=C5)CC4)=O)S(C6=CC=CC7=C6C=CN=C7)(=O)=O

    Synonyms

    KN62; KN-62; KN 62.


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    In Vitro

    In vitro activity: KN-62 suppresses the A23187-induced autophosphorylation of Ca2+/CaM kinase in PC12 D cells. KN-62 (10 μM) inhibits carbachol and potassium-stimulated insulin secretion from rat pancreatic islets. KN-62 also inhibits growth of K562 cells and blocks cell cycle progression.


    Kinase Assay: Total kinase activity of CaMKII, determined in a standard 2 min assay (100 μL), contained 35 mM HEPES, 10 mM MgCl2, 1 mM CaCl2, 10 μg of chicken gizzard myosin 20-kD light chain, 0.1 μM calmodulin, and 10 μM [γ-33]ATP at 30 °C. The kinase reaction is halted by adding 1 mL of 10% trichloroacetic acid.  


    Cell Assay: For cell growth analysis, K562 cells are plated in a 3-cm dish with 5 mL of culture medium containing various concentration of KN-62. After two days in these condition cell numbers are counted.

    In VivoKN-62 inhibits seizure-induced expression of brain-derived neurotrophic factor mRNA in adult rat brain.
    Animal modelSprague Dawley Rats
    Formulation & DosageDissolved in 0.5 mM KN-62/50% DMSO; 2 pmol; intracerebroventricular (ICV) injection
    References

    J Biol Chem. 1990 Mar 15;265(8):4315-20; Eur J Neurosci. 1998 Jan;10(1):377-87.


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

    KN-62

     

    KN-62



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