IMD 0354

製品コードS2864

IMD 0354化学構造

分子量(MW):383.67

IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.

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JPY 16900
JPY 20200
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バルク問合せ

カスタマーフィードバック(5)

  • (B) Histological examinations of xenograft lesions produced by A549 cells. We stained the lesions with H&E, TUNEL and staining for Ki-67. (C, D) The histogram shows percentage of A549 cells that were positive for proliferation marker Ki-67 and apoptosis marker TUNEL in 3 representative fields. Results are expressed as the mean ± SD. ns. P > 0.05, **P < 0.01 and ***P < 0.001 for the indicated comparisons by 1-way A OVA or Student’s t test.

    Int J Cancer, 2018, 144(1):200-209. IMD 0354 purchased from Selleck.

    (C) ELISA showed that the elevated IL-8 was significantly inhibited in HUVEC-shCD109 when pretreated with SB525334, LY294002, or IMD 0354. GAPDH served as a loading control for WB. Data shown as mean ± SD were from triplicates of three independent experiments. **P < 0.01 by t test. CM, conditioned media; NC, negative control.

    Oncotarget, 2016, 7(20):29333-45. IMD 0354 purchased from Selleck.

  • E. MΦ-THP-1 cells were pretreated with IMD 0354 (3μM) for 30 minutes, then incubated with core protein for 3 and 6 hours, cell lysates were analyzed by immunoblotting to examine the A20 expression.

    Oncotarget, 2016, 7(23):33796-808. IMD 0354 purchased from Selleck.

    Dystrophic muscle fibroblasts treated with 5 μM IMD-0354 or vehicle were incubated in serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) for 24 h. Cells containing EdU incorporated into the nucleus were scored as EdU-positive (D, up panel), and the percentage of EdU-positive cells was calculated (D, down panel). The scale bar is 50 μm. Values are expressed as the mean ± SD, n = 3. #P < 0.05 versus cells in grow medium (10% FBS); *P < 0.05 versus cells under serum deprivation without TGF-β1 and IMD-0354 treatments; **P < 0.05.

    Biochem Biophys Res Commun, 2016, 471(4):576-81. IMD 0354 purchased from Selleck.

  • IMD-0354 attenuates TGF-β1-mediated survival and proliferation in dystrophic muscle fibroblasts. (A) Dystrophic muscle fibroblasts were cultured in culture medium or serum-deprived medium with (+) or without (−) TGF-β1 (10 ng/ml) and various concentrations of IMD-0354 as indicated for 24 h. Cell viability was determined by CCK-8 assay. (B) Dystrophic muscle fibroblasts were cultured as described in A. Western blot analysis was applied to determine the protein abundance of cleaved caspase-3, cleaved PARP and Bcl-2. (C) Dystrophic muscle fibroblasts were cultured in culture medium or serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) and various concentrations of IMD-0354 as indicated for 24 h. The protein abundance of cyclin D1 and PCNA was determined by Western blot. (D) Dystrophic muscle fibroblasts treated with 5 μM IMD-0354 or vehicle were incubated in serum-deprived medium (1% FBS) with (+) or without (−) TGF-β1 (10 ng/ml) for 24 h. Cells containing EdU incorporated into the nucleus were scored as EdU-positive (D, up panel), and the percentage of EdU-positive cells was calculated (D, down panel). The scale bar is 50 μm. Values are expressed as the mean ± SD, n = 3. #P < 0.05 versus cells in grow medium (10% FBS); *P < 0.05 versus cells under serum deprivation without TGF-β1 and IMD-0354 treatments; **P < 0.05.

    Biochem Biophys Res Commun, 2016, 471(4):576-81.. IMD 0354 purchased from Selleck.

製品安全説明書

IκB/IKK阻害剤の選択性比較

生物活性

製品説明 IMD-0354 is an IKKβ inhibitor and blocks IκBα phosphorylation in NF-κB pathway.
ターゲット
IKKβ [1]
体外試験

IMD-0354 (< 5 μM) inhibits the expression of NF-κB as well as the translocation of NF-κB to the nucleus in HMC-1 cells. IMD-0354 suppresses cell proliferation in a time- and dose-dependent manner in HMC-1 cells. IMD-0354 (0.5 μM) almost inhibits the proliferation of IC-2G559 cells and IC-2V814 cells. IMD-0354 (0.5 μM) results in arrest of the cell cycle at the G0/G1 phase in HMC-1 cells. IMD-0354 (1 μM) increases the number of cells with hypodiploid DNA content in HMC-1 cells. IMD-0354 (<1 μM) decreases the ratio of cells in S and G2/M phases in HMC-1 cells. IMD-0354 (1 μM) downregulates Cyclin D3 expression as well as pRb phosphorylation level in a time-dependent manner in HMC-1 cells. IMD-0354 (< 10 μM) has no influence on the signals of STAT3 and STAT6, whereas the phosphorylation of STAT1 and STAT5 is very slightly suppressed at high concentrations in HMC-1 cells. IMD-0354 suppresses the translocation of NF-κB to the nucleus in CBhCMCs after 24 hours in a dose-dependent manner. [1] IMD-0354 inhibits 98.5% of NF-κB activity at a concentration of 10 μg/ml in HepG2 cells. [2] IMD-0354 (1 μM) ameliorates the TNFα-induced decrease in the adiponectin concentration in the media, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. IMD-0354 (1 μM) restores the phosphorylation of Akt down-regulated by the TNFα treatment, when the TNFα (6 nM) and insulin (100 nM) are administered simultaneously in 3T3-L1 adipocytes serum-starved for 12 h. [3] IMD-0354 (1 μM) inhibits phosphorylation of IκBα and nuclear translocation of nuclear factor-kappa B (NF-κB) induced by tumor necrosis factor-α (TNF-α) in cultured cardiomyocytes. IMD-0354 (1 μM) significantly reduces TNF-α-induced production of interleukin-1β and monocyte chemoattractant protein-1 from cultured cardiomyocytes. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HFF cells NVztd|ZLTnWwY4Tpc44h[XO|YYm= Mn3WO|IhcA>? MkH3RY51cWGyaXPvcZBt\XijbjDhZ5Rqfmm2eTDh[4FqdnO2IGTvfI9xdGG|bXGg[49v\GmrIGLIJJRi[2i7en;peIV{KGW6cILld5NqdmdieXXscI94KG[udX;y[ZNk\W62IIDyc5RmcW5iaX7m[YN1\WRiaX6gTGZHKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDmcJVwemW|Y3XuZ4Uh[XO|YYmsJGlEPTB;MD6wNVYh|ryP MUmyNlk4ODl|Nx?=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 IMD-0354 at 5 mg/kg also significantly decreases NF-κB, but the magnitude of the decrease is lower than with 20 mg/kg IMD-0354 in lungs of OVA-sensitized mice. IMD-0354 (20 mg/kg) ameliorates airway hyperresponsiveness and reduces the numbers of bronchial eosinophils and mucus-producing cells in OVA-sensitized mice. IMD-0354 (20 mg/kg) also reduces the total numbers of cells and eosinophils in bronchoalveolar lavage fluid in OVA-sensitized mice. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL)-5 and IL-13 and eotaxin in the airways and/or lungs of OVA-sensitized mice, but it does not affect the restoration of Th1 cytokines such as IL-12 and interferon-gamma under the same experimental conditions. IMD-0354 (20 mg/kg) results in a partial decrease in serum IgE concentration in OVA-sensitized mice. [2] IMD-0354 significantly decreases the plasma glucose levels in KKAy mice treated with and fed an HF diet in an dose-dependent manner without influence of body weight. [3] IMD-0354 (10 mg/kg) results in a significant dose-dependent reduction of the infarction area/area at risk ratio and the preservation of fractional shortening ratio. [4]

お薦めの試験操作(参考用のみ)

細胞試験: [1]
+ 展開
  • 細胞株: HMC-1, IC-2, CBhCMCs cells
  • 濃度: 10 μM
  • 反応時間: 72 hours
  • 実験の流れ: Cells (2×105 cells/mL) are incubated in phenol red free α-MEM containing 10% FCS (for HMC-1 and IC-2 cells) or 5% FCS (for CBhCMCs), and antibiotics with or without various concentrations of IMD-0354, STI571, or PDTC. IC-2WT cells and CBhCMCs are incubated in the presence of 100 ng/mL recombinant rat or recombinant human SCF. One hundred microliters of cell suspension is applied to each well of 96-well culture plates and are incubated for 24, 48, and 72 hours. Before 4 hours from the end of the culture, 10 μL of 5 mg/mL 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyl-tetrazolium bromide (MTT) dissolves in PBS is added to each well. The reaction is stopped with the addition of 100 μL of 10% SDS in 0.01 N HCl. Absorbance is measured at 577 nm with ImmunoMini NJ-2300.
    (参考用のみ)
動物試験:[2]
+ 展開
  • 動物モデル: ovalbumin (OVA)-sensitized mice
  • 製剤: 5% carboxymethylcellulose
  • 投薬量: 20 mg/kg
  • 投与方法: Intraperitoneal
    (参考用のみ)

溶解度 (25°C)

体外 Ethanol 77 mg/mL (200.69 mM)
DMSO 10 mg/mL (26.06 mM)
Water 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):
2% DMSO+5% Tween 80+0.5% CMC Na
混合させたのち直ちに使用することを推奨します。
3mg/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 383.67
化学式

C15H8ClF6NO2

CAS No. 978-62-1
保管
in solvent
別名 N/A

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

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

IκB/IKKシグナル伝達経路

IκB/IKK Inhibitors with Unique Features

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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