CAS NO: | 1188890-41-6 |
规格: | ≥98% |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 599.03 |
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Formula | C26H32ClN2O8PS |
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 |
Synonyms | KN-93 phosphate; KN93; KN 93; KN-93; |
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. |
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In Vivo | KN-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 model | Sprague Dawley female rats |
Formulation & Dosage | Dissolved in 4 μL of 0.9% physiological saline containing 0.02% ascorbic acid; 5 μg; Intrastriatal administration |
References | Biochem Biophys Res Commun. 1991 Dec 31;181(3):968-75; Neuropsychiatr Dis Treat. 2013;9:1213-20. |