Tideglusib

製品コードS2823 別名:NP031112, NP-12

Tideglusib化学構造

分子量(MW):334.39

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.

サイズ 価格(税別)  
JPY 30200
JPY 80000
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バルク問合せ

カスタマーフィードバック(5)

  • (A) NPCs were treated with 3µM of the GSK3 inhibitor (tideglusib) for 24 hours. Representative images of untreated SPG11-NPCs (SPG11‐NT) and tideglusib-treated SPG11-NPCs (SPG11-Tide) on day 3. Cell proliferation was analyzed using colabeling of PCNA in Nestin/Sox2-positive NPCs. Nuclei were visualized with DAPI. Scale bar = 50µm. (B) Increased numbers of Nestin/Sox2‐positive cells colabeled with PCNA in CHIR99021-treated SPG11-NPCs. (C) Tideglusib-treated SPG11-NPCs, compared to untreated NPCs, revealed restoration of cell proliferation similar to the CTRL‐NPCs.

    Ann Neurol, 2016, doi: 10.1002/ana.24633. Tideglusib purchased from Selleck.

    BV-2 cells were pretreated with NP-12 (an inhibitor of GSK-3β, 2.5 μM) for 4 h, following which they were treated with PLD for 1 h. After cells were harvested, the protein expression of GSK-3β, p-GSK-3βSer9 (D), and Nucleosol-Nrf2 (E) was measured via Western blotting.

    Front Immunol, 2018, 9:2527. Tideglusib purchased from Selleck.

  • (C) and Western blotting (D) analysis showed treatment with GSK3β inhibitors TWS119 (10 μM) and Tideglusib (1 μM) for 24 hours suppressed E-cadherin expression in FGF19 knockdown MHCC97H cells. All error bars in this figure represent S.E.M. (n = 3, **P < 0.01).

    Oncotarget, 2016, 7(12):13575-86. Tideglusib purchased from Selleck.

    (A) Merged confocal images of SPG11 and CTRL neurons generated from iPSCs and co-immunostained for βIII-tubulin (Tuj-1) and cleaved-caspase3 (cCasp3). Scale bar = 20 μm. (B) Representative images of TUJ-1 stained SPG11 and control neurons.

    Front Neurosci, 2018, 12:914. Tideglusib purchased from Selleck.

  • Isoform specificity of different chemical inhibitors of GSK3. Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3′-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.

    PLoS One, 2014, 9(7):e100947. . Tideglusib purchased from Selleck.

製品安全説明書

GSK-3阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
GSK-3β [1]
(Cell-free assay)
60 nM
体外試験

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]

アッセイ
Methods Test Index PMID
Western blot
KDM1A / Nestin / OCT4 / CD133 / Tuj-1; 

PubMed: 27501329     


GSC11 cells were treated with 2.5 µM or 5 µM tideglusib for 36 h, and cell lysates were assessed by immunoblotting. 

27501329
Growth inhibition assay
Cell viability; 

PubMed: 27501329     


(e) GSC11 and GSC20 cells were treated with different concentration of tideglusib for 7d. IC50 values for each cell line were calculated using the GraphPad Prism 6 software (mean ± s.e.m., n=3 independent experiments). (f) GSC11 and GSC20 cells were treated with dimethyl sulfoxide (DMSO), temozolomide (TMZ; 100 µM), tideglusib (2.5 µM), or TMZ plus tideglusib for the indicated times, and cell proliferation was assessed by XTT assays (mean ± s.e.m., n=3 independent experiments, paired Student’s t-test). P values were analyzed by comparing TMZ or tideglusib along versus the combination of the two and shown. 

27501329
体内試験 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]

お薦めの試験操作(参考用のみ)

動物試験:[3]
+ 展開
  • 動物モデル: Transgenic APPsw-tauvlw mice overexpressing human mutant APP and a triple human tau mutation.
  • 製剤: 26% peg400 (Polyethylene Glycol 400), 15% Chremophor EL and water
  • 投薬量: 200 mg/kg
  • 投与方法: Oral gavage
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 8 mg/mL (23.92 mM) warming
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
4% DMSO+corn oil
混合させたのち直ちに使用することを推奨します。
2.5mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 334.39
化学式

C19H14N2O2S

CAS No. 865854-05-3
保管
in solvent
別名 NP031112, NP-12

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03692312 Not yet recruiting Congenital Myotonic Dystrophy AMO Pharma Limited October 2018 Phase 2|Phase 3
NCT03692312 Not yet recruiting Congenital Myotonic Dystrophy AMO Pharma Limited October 2018 Phase 2|Phase 3
NCT02858908 Completed Myotonic Dystrophy 1 AMO Pharma Limited July 20 2016 Phase 2
NCT02858908 Completed Myotonic Dystrophy 1 AMO Pharma Limited July 20 2016 Phase 2
NCT02586935 Completed Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario Canada|St. Michael''s Hospital Toronto|University of Toronto|Anagnostou Evdokia M.D. February 10 2016 Phase 2
NCT02586935 Completed Autism Spectrum Disorders Evdokia Anagnostou|Holland Bloorview Kids Rehabilitation Hospital|McMaster University|University of Western Ontario Canada|St. Michael''s Hospital Toronto|University of Toronto|Anagnostou Evdokia M.D. February 10 2016 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 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.

GSK-3シグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID