1. MAPK/ERK Pathway
    Apoptosis
  2. MAP3K
    Apoptosis
  3. Takinib

Takinib (Synonyms: EDHS-206)

目录号: HY-103490 纯度: 99.15%
产品使用指南

Takinib (EDHS-206) 是一种有效且选择性的 TAK1 抑制剂 (IC50=9.5 nM),比 IRAK4 (IC50=120 nM) 和 IRAK1 (IC50=390 nM) 作用强 1.5 log 倍。Takinib 是一种TAK1自磷酸化的抑制剂,在 ATP 结合口袋内非竞争性结合。在类风湿关节炎和转移性乳腺癌细胞模型中,Takinib 诱导 TNF-α 刺激的细胞凋亡 (apoptosis)。Takinib 也是恶性疟原虫蛋白激酶 9 (PfPK9) 的抑制剂 (KD(app) of 0.46 nM)。

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Takinib Chemical Structure

Takinib Chemical Structure

CAS No. : 1111556-37-6

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Top Publications Citing Use of Products

    Takinib purchased from MCE. Usage Cited in: Mol Biol Cell. 2018 Oct 1;29(20):2470-2480.

    WT and WDR62-KO cells are pre-incubated withTakinib (2 µM) for 1 h then treated with TNFα (50 ng/mL) for 15 min. JNK activation is determined by Western blotting.

    查看 MAP3K 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM)[1][2][3].

    IC50 & Target[1]

    TAK1

    9.5 nM (IC50)

    IRAK4

    120 nM (IC50)

    IRAK1

    390 nM (IC50)

    GCK

    430 nM (IC50)

    CLK2

    430 nM (IC50)

    MINK1

    1.9 μM (IC50)

    体外研究
    (In Vitro)

    Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells[1].
    Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65[1].
    Takinib serves as a chemical starting point for the development of PfPK9 (KD(app) of 0.46 μM) inhibitors for malaria[3].
    Takinib (2 hours; 0.1-20 µM; human RASFs) induces phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727 in IL-1β-treated (10 ng/mL; 30 min) RASFs[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[1]

    Cell Line: Breast cancer cell line MDA-MB-231
    Concentration: 10 μM
    Incubation Time: 5, 15, 30, 60 minutes
    Result: IKK and p65 were maximally phosphorylated at 15 minutes, which indicated activation of the NF-κB pathway, while p38 phosphorylation peaks at 30 minutes.

    Western Blot Analysis[4]

    Cell Line: IL-1β-treated (10 ng/mL; 30 min) RASFs
    Concentration: 0.1-20 µM
    Incubation Time: 2 hours
    Result: Induced phosphorylation of TAK1Thr184/187, STAT3Tyr705 and STAT3Ser727.
    体内研究
    (In Vivo)

    Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis[4].
    Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice[5].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Male DBA/1 mice (CIA arthritis model)[4]
    Dosage: 50 mg/kg
    Administration: Intraperitoneally; daily from days 18-36
    Result: Showed a reduction in clinical arthritic score compared to vehicle control.
    Animal Model: Female NSG mice (8 weeks old)[5]
    Dosage: 50 mg/kg
    Administration: Oral gavage; daily until 17 days
    Result: Slowed tumor growth and reduced tumor size/weight.
    分子量

    322.36

    Formula

    C18H18N4O2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 50 mg/mL (155.11 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.1021 mL 15.5106 mL 31.0212 mL
    5 mM 0.6204 mL 3.1021 mL 6.2042 mL
    10 mM 0.3102 mL 1.5511 mL 3.1021 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (7.76 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (7.76 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 2.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (7.76 mM); Suspended solution; Need ultrasonic

      此方案可获得 2.5 mg/mL (7.76 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献
    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    Takinib
    目录号:
    HY-103490
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