KN-93

製品コードS6787 バッチS678702

印刷

化学情報

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

C26H29ClN2O4S
分子量 501.04 CAS No. 139298-40-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.58 mM)
Ethanol 50 mg/mL (99.79 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
5% DMSO 95% Corn oil
1.65mg/ml
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/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 is a cell-permeable, reversible and competitive inhibitor of Ca2+/calmodulin-dependent protein kinase II (CaMK-II) with Ki of 2.58 μM at rabbit myocardial CaM kinase activity.
in vitro

KN-93, a CaMK2 inhibitor, reduces the B-cell differentiation and IgG production by differentiated plasma cells, and inhibits Blimp-1 expression in B cells.[2]
in vivo

KN93 shows the protective effect on acute pancreatitis (AP) at a dose-dependent way, with no toxic side effects on the mice.[3]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 human B cells isolated from lupus nephritis (LN) patients
濃度 5 μM
反応時間 --
実験の流れ

For B-cell differentiation, isolated naive B cells were cultured in Roswell Park Memorial Institute (RPMI) 1640 supplemented with 10% fetal bovine serum (FBS) and 1% penicillin/streptomycin. Cells were stimulated with antihuman IgM (5 μg/ml) and antihuman CD40 (1 μg/ml) antibodies in the presence of interleukin (IL)-2 (20 ng/ml), IL-4 (25 ng/ml) and IL-21 (50 ng/ml) for 8 days. For signaling study, cells treated with KN-93 (1 μM) to study the roles of CaMK2 in human B-cell differentiation. Proteins were loaded to sodium dodecyl sulfate (SDS)-polyacrylamide gels and electrotransferred onto polyvinylidine difluoride membranes after separation. Membranes were blocked with 5% bovine serum albumin in TBST buffer and incubated with primary antibodies against ORAI1, ORAI2, STIM2, Blimp-1, and p-CaMK2, at 4°C overnight. Membranes were incubated with anti-GAPDH primary antibody and used as internal control. Membranes were then washed with TBST and incubated with horseradish-peroxidase-conjugated antirabbit or antimouse IgG at room temperature for 60 min. Signals were detected by enhanced chemiluminescence analysis kit.
動物実験 動物モデル mice of acute pancreatitis (AP) model
投薬量 5, 10, 20 mg/kg
投与方法 i.p.

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：

CaMK4 controls follicular helper T cell expansion and function during normal and autoimmune T-dependent B cell responses [ Nat Commun, 2024, 15(1):840] PubMed: 38287012
Kisspeptin-10 binding to Gpr54 in osteoclasts prevents bone loss by activating Dusp18-mediated dephosphorylation of Src [ Nat Commun, 2024, 15(1):1300] PubMed: 38346942
CaMKII regulates the proteins TPM1 and MYOM2 and promotes diacetylmorphine-induced abnormal cardiac rhythms [ Sci Rep, 2023, 13(1):5827] PubMed: 37037889
Late sodium current in synergism with Ca2+/calmodulin-dependent protein kinase II contributes to β-adrenergic activation-induced atrial fibrillation [ Philos Trans R Soc Lond B Biol Sci, 2023, 378(1879):20220163] PubMed: 37122215
SGLT2 inhibitor dapagliflozin reduces endothelial dysfunction and microvascular damage during cardiac ischemia/reperfusion injury through normalizing the XO-SERCA2-CaMKII-coffilin pathways [ Theranostics, 2022, 12(11):5034-5050] PubMed: 35836807
Silica nanoparticles induce cardiac injury and dysfunction via ROS/Ca2+/CaMKII signaling [ Sci Total Environ, 2022, 837:155733] PubMed: 35526619
Activation of transient receptor potential vanilloid 4 is involved in pressure overload-induced cardiac hypertrophy [ Elife, 2022, 11e74519] PubMed: 35731090
Ion channel Piezo1 activation promotes aerobic glycolysis in macrophages [ Front Immunol, 2022, 13:976482] PubMed: 36119083
Effects and potential mechanism of Ca2+/calmodulin‑dependent protein kinase II pathway inhibitor KN93 on the development of ovarian follicle [ Int J Mol Med, 2022, 50(4)121] PubMed: 35929517
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

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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