Tideglusib

別名：NP031112, NP-12

製品コード：S2823 純度：99.93%

Tideglusib is an irreversible, non ATP-competitive GSK-3β inhibitor with IC50 of 60 nM in a cell-free assay; fails to inhibit kinases with a Cys homologous to Cys-199 located in the active site. Phase 2.

CAS No. 865854-05-3

サイズ	価格(税別)	在庫状況
50mg	JPY 25500	国内在庫あり
200mg	JPY 70500	国内在庫あり
5g	JPY 298500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（27）

カスタマーフィードバック5个实验数据

製品安全説明書

現在のバッチを見る：純度： 99.93%

99.93

Tideglusib関連製品

関連ターゲット	GSK-3α GSK-3β	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

GSK-3シグナル伝達経路

GSK-3阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
SH-SY5Y	Function assay	10 uM	1 hrs	Inhibition of GSK-3beta in human SH-SY5Y cells assessed as reduction in amyloid beta (25 to 35) -induced toxicity at 10 uM pre-incubated for 1 hrs before amyloid beta (25 to 35) addition and measured after 72 hrs post Abeta25-35 addition by MTT assay	29208522
SH-SY5Y	Function assay	30 uM	1 hrs	Inhibition of GSK-3beta in human SH-SY5Y cells assessed as reduction in amyloid beta (25 to 35) -induced toxicity at 30 uM pre-incubated for 1 hrs before amyloid beta (25 to 35) addition and measured after 72 hrs post Abeta25-35 addition by MTT assay	29208522
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生物活性

製品説明

Targets

GSK-3β ^[1]
(Cell-free assay)

60 nM

In Vitro
In vitro	Tideglusib irreversibly inhibits GSK-3, reduces tau phosphorylation, and prevents apoptotic death in human neuroblastoma cells and murineprimary neurons. ^[1] Tideglusib (2.5 μM) inhibits glutamate-induced glial activation as evidenced by decreased TNF-α and COX-2 expression in rat primary astrocyte or microglial cultures. Tideglusib (2.5 μM) also exerts a potent neuroprotective effect on cortical neurons from glutamate-induced excitotoxicity as evidenced by significant reduction in the number of Annexin-V-positive cells in rat primary astrocyte or microglial cultures. ^[2]
Kinase Assay	Binding Experiments with Radiolabeled Tideglusib
Kinase Assay	[³⁵S]Tideglusib (207 Bq/nmol) at 55 μM is incubated with 5 μM GSK-3β for 1 h at 25 °C in 315 μL of 50 mM Tris-HCl, pH 7.5, containing 150 mM NaCl and 0.1 mM EGTA. The incubation is extended for another 30 min after having added 35 μL of the same buffer with or without 100 mM DTE. Finally, a third 40-μL aliquot of each original sample is mixed with 10 μL of denaturing electrophoresis sample buffer without reducing agents, and 35 μL of this mixture is loaded onto a 10% polyacrylamide gel and subjected to SDS-PAGE, followed by fluorography of the dried gel.
細胞実験	細胞株	Miapaca2 cells
	濃度	5 μM
	反応時間	24 h
	実験の流れ	Cells were treated with indicated concentration of drug for 24 h.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	KDM1A / Nestin / OCT4 / CD133 / Tuj-1		27501329
	Growth inhibition assay	Cell viability		27501329

In Vivo
In Vivo	Tideglusib (50 mg/kg) injected into the adult male Wistar rats hippocampus dramatically reduces kainic acid-induced inflammation and has a neuroprotective effect in the damaged areas of the hippocampus. ^[2] Tideglusib (200 mg/kg, oral) results in lower levels of tau phosphorylation, decreased amyloid deposition and plaque-associated astrocytic proliferation, protection of neurons in the entorhinal cortex and CA1 hippocampal subfield against cell death, and prevention of memory deficits in APP/tau double transgenic mice. ^[3]
動物実験	動物モデル	Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
	投与量	200 mg/kg
	投与経路	Oral gavage

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02586935	Completed	Autism Spectrum Disorders	Evdokia Anagnostou\|Holland Bloorview Kids Rehabilitation Hospital\|McMaster University\|University of Western Ontario Canada\|Unity Health Toronto\|University of Toronto\|Anagnostou Evdokia M.D.	February 10 2016	Phase 2

参考
[1] Domínguez JM, et al. J Biol Chem, 2012, 287(2), 893-90 [2] Luna-Medina R, et al. J Neurosci, 2007, 27(21), 5766-5776. [3] Seren?L, et al. Neurobiol Dis, 2009, 35(3), 359-367. [4] Zalyte E, et al. Int J Mol Med. 2022 Jun;49(6):84. + 展開

参考

[4] Zalyte E, et al. Int J Mol Med. 2022 Jun;49(6):84.

+ 展開

化学情報

分子量	334.39	化学式	C₁₉H₁₄N₂O₂S
CAS No.	865854-05-3	SDF	Download Tideglusib SDFをダウンロードする
Smiles	C1=CC=C(C=C1)CN2C(=O)N(SC2=O)C3=CC=CC4=CC=CC=C43
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 1 mg/mL ( (2.99 mM)； Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	4%DMSO 1 Corn oil	2.5mg/ml	Taking the 1 mL working solution as an example, add 40 μL of 62.5 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5% DMSO 1 95% Corn oil	1.25mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	1.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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* 必須

よくある質問（FAQ）

質問1:
I want to deliver S2823 via i.p. injection, can you suggest one?

回答
This compound can be dissolved in 4% DMSO+corn oil at 2.5 mg/ml clearly. This is the highest concentration, since its solubility in DMSO is pretty low.

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