KN-93 Phosphate

製品コードS7423 バッチS742301

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26 H29 Cl N2 O4 S . H3 O4 P
分子量 599.03 CAS No. 1188890-41-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (166.93 mM)
Water 92 mg/mL (153.58 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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]

プロトコル(参考用のみ)

キナーゼアッセイ Measurement of activities of autophosphorylated/non-autophosphorylate CaMKII
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.
動物実験 動物モデル Sprague Dawley female rats
投薬量 ~5 μg
投与方法 Intrastriatal administration

参考

  • https://pubmed.ncbi.nlm.nih.gov/1662507/
  • https://pubmed.ncbi.nlm.nih.gov/8519682/
  • https://pubmed.ncbi.nlm.nih.gov/20023417/
  • https://pubmed.ncbi.nlm.nih.gov/23983471/
  • https://pubmed.ncbi.nlm.nih.gov/24829059/

カスタマーフィードバック

Data from [Data independently produced by , , Cell Biosci, 2016, 6:37.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

SERCA-mediated endoplasmic reticulum stress facilitates hematopoietic stem cell mobilization [ Stem Cell Res Ther, 2025, 16(1):208] PubMed: 40275396
Bacterial ubiquitin ligase engineered for small molecule and protein target identification [ bioRxiv, 2025, 2025.03.20.644192] PubMed: 40166235
An L-type calcium channel blocker nimodipine exerts anti-fibrotic effects by attenuating TGF-β1 induced calcium response in an in vitro model of thyroid eye disease [ Eye Vis (Lond), 2024, 11(1):37] PubMed: 39237996
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

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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