BIX 02189

製品コードS1531

BIX 02189化学構造

分子量(MW):440.54

BIX02189は一種の選択性的なMEK5阻害剤で、無細胞試験でIC50値が1.5 nMですが、ERK5触媒活性も抑制して、このIC50値が59 nMになりますが、密接関連のキナーゼMEK1、MEK2、ERK2とJNK2を抑制しません。

サイズ 価格 在庫  
JPY 43196.40 あり
JPY 24477.96 あり
JPY 46076.16 あり
JPY 139668.35 あり

カスタマーフィードバック(7)

  • J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

    Inhibition of ERK5 suppresses Nrf2 nuclear translocation in mouse aorta in vivo. Nrf2 nuclear translocation in mouse aortic endothelium was analyzed by en face immunofluorescence staining assay using anti-Nrf2 antibody (red). Mice were treated with either 10 mg/kg of BIX02189 (in 25% DMSO) or vehicle control (same volume of 25% DMSO) by ntraperitoneal injection. Endothelium of thoracic aorta was stained with anti-vascular endothelial-cadherin (VE-cadherin) antibody for endothelial cell-cell junction staining (green), Topro3 for nuclear staining (blue), and anti-Nrf2 antibody (red) and photographed under a confocal microscope..

    J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

  • Inhibition of ERK5 suppresses laminar flow-mediated Nrf2-dependent gene expression. B, HUVECs were exposed to atheroprotective flow for 16–24 h in the presence of either DMSO or BIX02189 (10uM). Protein expression of HO-1, NQO1, eNOS, pERK5, ERK5, and tubulin was determined by immunoblotting with specific antibodies. Data are representative from three independent experiments.

    J Biol Chem 2012 287, 40722-31. BIX 02189 purchased from Selleck.

    Effects of BIX02189 on cadmium-induced apoptosis in HK-2 cells. (A) PARP cleavage. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with 0, 20, or 50 lM CdCl2 for 16 h. Cell lysates were subjected to Western immunoblotting using antibodies against PARP and actin. Full-length and cleaved forms of PARP were detected at 116- and 89-kDa, respectively. Results are representative of at least four experiments. (B) Cytoplasmic nucleosomes. Cells were preincubated with 0.1% DMSO or 20 lM BIX02189 for 1 h, then incubated with or without 20 lM CdCl2 for 16 h. The cytoplasmic fraction was used for a nucleosomes ELISA. Each value (mean ± S.E.M., n = 5–7) represents the fold increase with respect to untreated control (without BIX02189 or CdCl2). Results are representative of four experiments.

    Biochem Biophys Res Commun 2012 421, 490–493. BIX 02189 purchased from Selleck.

  • Effects of BIX02189 on cadmium-induced accumulation of phosphorylated ERK5, phosphorylated ERK1/2, phosphorylated CREB, and c-Fos proteins in HK-2 cells. Cells were preincubated with 0.1% DMSO or 5, 10, 20, or 50 uM BIX02189 for 1 h, then incubated with or without 50 uM CdCl2 for 2 (top four panels) or 4 h (bottom four panels). Cell lysates were subjected to Western immunoblotting using antibodies against phospho-ERK5, ERK5, phospho-ERK1/2, ERK1/2, phospho-CREB, CREB, c-Fos, and actin. Results are representative of at least three experiments.

    Biochem Biophys Res Commun 2012 421, 490–493. BIX 02189 purchased from Selleck.

    Expression of iNOS, Fra-1, Fra-2, JunB, JunD, and FosB in PMN. (A) PMN were treated with or without SB203580 (40 μM), BIX02189 (30 μM), or SP600125 (40 μM) for 1 h before addition of NDMA (0.74 μg/μl). The cytoplasmic and nuclear fractions obtained from the cells were used to detect iNOS, Fra-1, Fra-2, JunB, JunD, and FosB protein levels by Western blot. The results shown are representative of five independent experiments.

    J IMMUNOTOXICOL 2013 10, 32-39. BIX 02189 purchased from Selleck.

  • T47D cells were pretreated 30 minutes BIX 02189(0,10,20,30,50 μM) and then co-incubated with Heregulin + BIX 02189 for 15 minutes.

    Dr. Franco Izzo of Institute of Biology and Experimental Medicine. BIX 02189 purchased from Selleck.

製品安全説明書

MEK阻害剤の選択性比較

生物活性

製品説明 BIX02189は一種の選択性的なMEK5阻害剤で、無細胞試験でIC50値が1.5 nMですが、ERK5触媒活性も抑制して、このIC50値が59 nMになりますが、密接関連のキナーゼMEK1、MEK2、ERK2とJNK2を抑制しません。
ターゲット
MEK5 [1]
(Cell-free assay)
ERK5 [1]
(Cell-free assay)
TGFβR1 [1]
(Cell-free assay)
MEK1 [1]
(Cell-free assay)
MEK2 [1]
(Cell-free assay)
1.5 nM 59 nM 580 nM >6.2 μM >6.2 μM
体外試験

BIX02189 blocks MEK5 and ERK5 catalytic activity with IC50 values of 1.5 nM and 59 nM, respectively. They are more potent than the effect caused by BIX02188 with IC50 values of 4.3 nM and 810 nM, respectively. BIX02189 shows inhibitory activity against CSF1R (FMS) with IC50 of 46 nM but displays no activity against related kinases MEK1, MEK2, ERK1, p38α, JNK2, EGFR, and STK16 with IC50 values of >3.7 μM. Pretreatment with BIX02189 inhibits sorbitol-induced phosphorylation of ERK5 in HeLa cells in a dose dependent manner, and displays no inhibitory activity against the phosphorylation of ERK1/2, p38, and JNK1/2 MAPKs. Treatment with only BIX02189 for 24 hours in HeLa or HEK293 cells does not show any cytotoxic effect. BIX02189 inhibits MEK5/ERK5/MEF2C-driven luciferase expression in HeLa and HEK293 cells with IC50 values of 0.53 μM and 0.26 μM, respectively. This is a more significant than the effect caused by BIX02188. [1] BIX02189 inhibits the activation of ERK5, and suppresses C-terminus of Hsc70-interacting protein (CHIP) mediated p53 ubiquitination, leading to the reverse of the protective effect caused by laminar flow (L-flow) in human umbilical vein endothelial cells (HUVECs) exposed to 15d-PGJ2. [2] BIX02189 (10 uM) inhibits ERK5 phosphorylation, and reduces myocyte enhancer factor 2 (MEF2) transcriptional activity in neonatal rat cardiomyocytes (NRCMs) stimulated by isoproterenol. BIX02189 enhances the sorbitol induced apoptosis in NRCMs, confirming the protective role of ERK5 in cardiomyocytes. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HeLa cells MX;GeY5kfGmxbjDhd5NigQ>? NEn1W5NKdmirYnn0bY9vKG:oIFXST|UheGixc4Doc5J6dGG2aX;uJIlvKHOxcnLpeI9tNXO2aX31cIF1\WRiaIXtZY4hUGWOYTDj[YxteyxiSVO1NF0xNjB3OTFOwG0> NFXGb2EzOzZ3NkSwOy=>

多くの細胞株試験データを見る場合、クリックしてください

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

Catalytic assay:

MEK5 protein isolated from the baculovirus expression system is used to measure kinase activity utilizing PKLight ATP Detection Reagent. The assay is performed using 15 nM GST-MEK5 and 0.75 μM ATP in assay buffer consisting of 25 mM Hepes, pH 7.5, 10 mM MgCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 μM Na3VO4, 0.5 mM DTT and 1% DMSO in the presence of varying concentrations of BIX02189. The kinase reaction mixture is incubated for 90 minutes at room temperature followed by addition of 10 μL of ATP detection reagent for 15 minutes. The relative light unit (RLU) signal is measured and the RLU signals are converted to percent of control (POC) values for the determination of IC50 value.
細胞試験:

[1]

+ 展開
  • 細胞株: HeLa cells
  • 濃度: Dissolved in DMSO, final concentration ~10 μM
  • 反応時間: Pretreatment for 1.5 hours
  • 実験の流れ:

    The cells are serum starved for 20 hours prior to stimulation with sorbitol at a final concentration of 0.4 M for 20 minutes at 37 °C. BIX02189 is added 1.5 hours prior to the addition of sorbitol. The cells are harvested and lysed in 50 μL RIPA buffer containing Halt protease and phosphate inhibitors at 4 °C for 5-10 minutes. The lysates are centrifuged for 10 minutes at 14,000 rpm and 50 μL lysate is added to 50 μl 2× sample buffer and boiled for 4 minutes at 95 °C. Twenty microliters sample is run on SDS–PAGE 10% Tris-glycine gels and transferred to nitrocellulose. Western blotting is done with appropriate antibodies.


    (参考用のみ)

溶解度 (25°C)

体外 Ethanol 80 mg/mL (181.59 mM)
DMSO 60 mg/mL warmed (136.19 mM)
Water Insoluble
体内 順序で溶剤を入れること:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
10mg/mL

* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)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 440.54
化学式

C27H28N4O2

CAS No. 1094614-85-3
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

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

技術サポート

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

Handling Instructions

他の質問がある場合は、お気軽くお問合せください。

  • * 必須

よくある質問(FAQ)

  • 問題1:

    I would like to perform some in vivo experiments in immunodeficient mice. how to perform the experiment in the best way? How to reconstitute the compound for in vivo experiments?

  • 回答:

    We suggest the following vehicle for BIX02189: 30% PEG400+0.5% Tween80+5% Propylene glycol, you can make a suspension at up to 30mg/ml that can be used for oral gavage. Or for i.p. injection, S1531 BIX 02189 can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 10 mg/ml clearly.

MEK信号経路図

MEK 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