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    KN-93 Phosphate
    KN-93 Phosphate

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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 #: V1299
    CAS #: 1188890-41-6Purity ≥98%

    Description: KN-93 Phosphate (KN 93; KN93), the phosphate salt of KN-93, is a potent, cell-permeable and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with potential anti-Parkinson's disease and anticancer activity. It inhibits CaMKII with a Ki of 0.37 μM, and showed no effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 suppresses ventricular arrhythmia induced by LQT2 without decreasing TDR. KN-93 inhibits androgen receptor activity and induces cell death irrespective of p53 and Akt status in prostate cancer. KN-93 ameliorates levodopa-induced dyskinesia in a rat model of Parkinson's disease. KN-93 protects rat cerebral cortical neurons from N-methyl-D-aspartic acid-induced injury. 

    References: Biochem Biophys Res Commun. 1991 Dec 31;181(3):968-75; Neuropsychiatr Dis Treat. 2013;9:1213-20.

    Related CAS #: 1188890-41-6 (phosphate); 139298-40-1 (free base); 1913269-12-1

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    Molecular Weight (MW)599.03
    CAS No.1188890-41-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (166.9 mM)
    Water: 92 mg/mL (153.6 mM)
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: (E)-N-(2-(((3-(4-chlorophenyl)allyl)(methyl)amino)methyl)phenyl)-N-(2-hydroxyethyl)-4-methoxybenzenesulfonamide phosphate

    SMILES Code: O=S(C1=CC=C(OC)C=C1)(N(C2=CC=CC=C2CN(C/C=C/C3=CC=C(Cl)C=C3)C)CCO)=O.O=P(O)(O)O


    KN-93 phosphate; KN93; KN 93; KN-93; 

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    In Vitro

    In vitro activity: KN-93 inhibits dopamine formation in PC12h cells by modulating the reaction rate of TH to reduce the Ca(2+)-mediated phosphorylation levels of the TH molecule. KN-93 inhibits serum-induced fibroblast cell growth with IC50 of 8 μM, and induces apoptosis after prolonged G1 arrest. KN-93 inhibits androgen receptor activity and p53-independently induces cell death in PCa cells.

    Kinase Assay: CaMKII activity is measured utilizing syntideII as a substrate. Purified CaMKII is pre-incubated in the assay mixture ( 35 mM Hepes-Na ( pH 8.0 ), 10 mM MgC12, 0.5 μM CaM, 5 μM ATP, 1 mM CaCl2 or 1 mM EGTA, total 25 μL) at 30 °C for 2 minutes. After this pre-incubation, the protein substrate/radioactive ATP mixture is added to the same test tube and the preparation is further incubated at 30 °C, for 5 minutes ( final assay condition; 35 mM Hepes-Na (pH 8.0), 10 mM MgCl2, 0.125 μM CaCl2, 20 μM syntideII, 11.25 μM [ γ-32P] ATP, 10 % DMSO and indicated concentrations of KN-93, supplemented with 0.25 mM CaCl2 and 2 mM EGTA (for autophosphorylated samples) or 0.25 mM EGTA and 2 mM CaCl2 (for nonautophosphorylated samples ), total 100 μL ). The reaction is terminated by adding of 25 μL of 100 % ( w/v ) ice-cold TCA. After centrifugation, 80 μL of the supernatant is applied to phosphocellulose paper. The filters are then washed with 75 mM H3P04 for 15 min with continuous agitation. After 4-cycles of washing, the radioactivity retains on the filter paper is quantified in a liquid scintillation counter.

    Cell Assay: NIH 3T3 fibroblasts are cultured on polystyrene dishes in DMEM and fetal bovine serum, supplemented with penicillin/streptomycmn in a 5% CO2 humidified chamber at 37°C. Cell growth is measured by using the MTT dye reduction method.

    In VivoKN-93 (5 μg) ameliorates levodopa-induced dyskinesia by lowering the expression of pGluR1S845 in a rat model of Parkinson’s disease. In MRL/lpr Foxp3-GFP mice, KN-93 results in a significant induction of Treg cells in the spleen, peripheral lymph nodes and peripheral blood, and decreases skin and kidney damage.
    Animal modelSprague Dawley female rats
    Formulation & DosageDissolved in 4 μL of 0.9% physiological saline containing 0.02% ascorbic acid; 5 μg; Intrastriatal administration

    Biochem Biophys Res Commun. 1991 Dec 31;181(3):968-75; Neuropsychiatr Dis Treat. 2013;9:1213-20.

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

    KN-93 Phosphate

    KN-93 had no antiparkinsonian effect on PD rats.

    KN-93 Phosphate

    KN-93 treatment reduced levodopa-induced dyskinesia in PD rats. Neuropsychiatr Dis Treat. 2013;9:1213-20.
    KN-93 Phosphate
    Intrastriatal KN-93 treatment reduced pGluR1S845 levels in PD rats. Total protein levels and membrane levels of GluR1 were decreased in PD rats. Neuropsychiatr Dis Treat. 2013;9:1213-20.

    KN-93 Phosphate

    Intrastriatal KN-93 treatment reduced the expression of Gad1 (A) and Nur77 (B) in PD rats. 6-OHDA lesions induced increased Gad1 and Nur77 in PD rats. Neuropsychiatr Dis Treat. 2013;9:1213-20.


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