KN-93

製品コードS6787 バッチS678702

印刷

化学情報

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）

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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (9.98mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	1.650mg/ml (3.29mM)

* <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は、ウサギ心筋CaMキナーゼ活性に対するKiが2.58 μMである、細胞透過性、可逆性、競合性のCa2+/カルモジュリン依存性プロテインキナーゼII（CaMK-II）阻害剤です。
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.
in vivo	KN93 shows the protective effect on acute pancreatitis (AP) at a dose-dependent way, with no toxic side effects on the mice.

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.

参考

https://pubmed.ncbi.nlm.nih.gov/9864285/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8569388/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8612788/

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：

TRPA1 exacerbates selective retinal ganglion cell vulnerability under acute ocular hypertension [ Acta Neuropathol Commun, 2025, 13(1):70]	PubMed: 40186313
Mechanosensor Piezo1‑mediated smooth muscular cell pyroptosis contributes to vascular calcification [ Int J Mol Med, 2025, 56(5)196]	PubMed: 40937566
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
In vitro and in vivo inhibition of the host TRPC4 channel attenuates Zika virus infection [ EMBO Mol Med, 2024, 10.1038/s44321-024-00103-4]	PubMed: 39009885
CaMKII suppresses proteotoxicity by phosphorylating BAG3 in response to proteasomal dysfunction [ EMBO Rep, 2024, 25(10):4488-4514]	PubMed: 39261742
The Role of Sodium Fluoride Mouthwash in Regulating FGF-2 and TGF-β Expression in Human Gingival Fibroblasts [ Biomedicines, 2024, 12(8)1727]	PubMed: 39200192
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

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。