受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26 H29 Cl N2 O4 S . H3 O4 P |
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分子量 | 599.03 | CAS No. | 1188890-41-6 | |
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (166.93 mM) | |
Water | 100 mg/mL (166.93 mM) | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | KN-93 Phosphate is a potent and specific inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMKII) with Ki of 0.37 μM, no remarkable inhibitory effects on APK, PKC, MLCK or Ca2+-PDE activities. KN-93 attenuates CaMKII-induced autophagy.This product is not soluble in saline. Please do not dissolve it in saline for administration. |
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in vitro | 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. [1] KN-93 inhibits serum-induced fibroblast cell growth with IC50 of 8 μM, and induces apoptosis after prolonged G1 arrest. [2] KN-93 inhibits androgen receptor activity and p53-independently induces cell death in PCa cells. [3] |
in vivo | KN-93 (5 μg) ameliorates levodopa-induced dyskinesia by lowering the expression of pGluR1S845 in a rat model of Parkinson’s disease. [4] 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. [5] |
キナーゼアッセイ | Measurement of activities of autophosphorylated/non-autophosphorylate CaMKII | |
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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. | ||
細胞アッセイ | 細胞株 | NIH 3T3 fibroblasts |
濃度 | ~24 μM | |
反応時間 | 70 hours | |
実験の流れ | 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 癈. Cell growth is measured by using the MTT dye reduction method. |
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動物実験 | 動物モデル | Sprague Dawley female rats |
投薬量 | ~5 μg | |
投与方法 | Intrastriatal administration |
Data from [Data independently produced by , , Cell Biosci, 2016, 6:37.]
Porcine reproductive and respiratory syndrome virus infection triggers autophagy via ER stress-induced calcium signaling to facilitate virus replication [ PLoS Pathog, 2023, 19(3):e1011295] | PubMed: 36972295 |
CaMKII may regulate renal tubular epithelial cell apoptosis through YAP/NFAT2 in acute kidney injury mice [ Ren Fail, 2023, 45(1):2172961] | PubMed: 36718671 |
Brain milieu induces early microglial maturation through the BAX-Notch axis [ Nat Commun, 2022, 13-1:6117] | PubMed: 36253375 |
Amino acid starvation-induced LDLR trafficking accelerates lipoprotein endocytosis and LDL clearance [ EMBO Rep, 2022, e53373] | PubMed: 34994492 |
Wnt 5a mediated inflammatory injury of renal tubular epithelial cells dependent on calcium signaling pathway in Trichloroethylene sensitized mice [ Ecotoxicol Environ Saf, 2022, 243:114019] | PubMed: 36030685 |
Intrinsic cardiac adrenergic cells contribute to LPS-induced myocardial dysfunction [ Commun Biol, 2022, 5(1):96] | PubMed: 35079095 |
N-Methyl D-aspartate receptor subtype 2B/Ca2+/calmodulin-dependent protein kinase II signaling in the lateral habenula regulates orofacial allodynia and anxiety-like behaviors in a mouse model of trigeminal neuralgia [ Front Cell Neurosci, 2022, 16:981190] | PubMed: 36187288 |
Terfenadine resensitizes doxorubicin activity in drug-resistant ovarian cancer cells via an inhibition of CaMKII/CREB1 mediated ABCB1 expression [ Front Oncol, 2022, 12:1068443] | PubMed: 36439493 |
Effect of feeding regimen on circadian activity rhythms of food anticipatory by ghrelin hormone in a pig model [ Nutr Neurosci, 2022, 1-19] | PubMed: 35249475 |
Chai-Hu-San-Shen Capsule Ameliorates Ventricular Arrhythmia Through Inhibition of the CaMKII/FKBP12.6/RyR2/Ca2+ Signaling Pathway in Rats with Myocardial Ischemia [ Evid Based Complement Alternat Med, 2022, 2022:2670473] | PubMed: 36225189 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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