1. NF-κB Autophagy
  2. IKK LRRK2
  3. IKK 16

IKK 16 是一种选择性的 IκB 激酶 (IKK) 抑制剂,作用于 IKK2IKK complexIKK1IC50 分别为 40 nM,70 nM 和 200 nM。IKK 16 还抑制富亮氨酸重复激酶 2 (LRRK 2),IC50 为 50 nM。

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IKK 16 Chemical Structure

IKK 16 Chemical Structure

CAS No. : 873225-46-8

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10 mM * 1 mL in DMSO ¥1100
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1 mg ¥400
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5 mg ¥990
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10 mg ¥1438
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100 mg ¥6988
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Top Publications Citing Use of Products

    IKK 16 purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Apr 3;10(4):304.   [Abstract]

    IKK 16 treatment overwhelms the function of CT55 to promote the activation of p65 and IκBα degradation. HCT116 cells transfected with Flag-CT55 were treated with IKK 16 (20 mM) or DMSO for 2 h before TNF-α treatment. Western blotting is performed to detect the protein levels of IκBα, p-p65, and p65.

    IKK 16 purchased from MCE. Usage Cited in: Mol Immunol. 2018 Nov 13;104:69-78.  [Abstract]

    Western analysis of proteins expression with treatment of IKK-16 or MG-132.

    IKK 16 purchased from MCE. Usage Cited in: Respir Res. 2017 Sep 20;18(1):174.  [Abstract]

    BECs are pretreated with specific STAT6 inhibitor (AS1517499) or a selective IκB kinase inhibitor (IKK 16) for half an hour, then treated for 24 h in the presence or absence of 20 ng/mL IL-4. Immunofluorescence staining of MUC5AC protein is performed according to the Methods.

    查看 IKK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.

    IC50 & Target[1]

    IKK2

    40 nM (IC50)

    IKK1

    200 nM (IC50)

    IKK

    70 nM (IC50)

    LRRK2

    50 nM (IC50)

    体外研究
    (In Vitro)

    IKK 16 是一种有效的 IKK2 抑制剂,IC50 值为 40 nM[1]IKK 16 是一种富含亮氨酸的repeat kinase-2 (LRRK2) 激酶抑制剂,其体外 IC50 为 50 nM。IKK 16 在体外对 LRRK2 表现出亚微摩尔 IC50 浓度,低于观察到的 Ser935 磷酸化细胞抑制作用。IKK 16 (20 μM) 可以在体外抑制 HEK293 GFP-LRRK2 G2019S 细胞 (GS) 或 A2016T/G2019S (IRM) 细胞中的 LRRK2 Ser935 磷酸化[1]

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

    体内研究
    (In Vivo)

    IKK 16 还在细胞因子释放的急性模型中表现出显著的体内活性。IKK 16 (30 mg/kg,sc) 或 (30 mg/kg,po) 在指定剂量下的两种给药途径均导致 86% (sc) 和 75% (po) 的显著抑制。IKK 16 (10 mg/kg,sc) 在小鼠的巯基乙酸盐诱导的腹膜炎模型中也有活性。该模型对中性粒细胞外渗的最大抑制约为 50%[1]。用 IKK 16 (1 mg/kg, iv) 处理脓毒症小鼠导致肝脏中 Akt 和 eNOS 上丝氨酸残基的磷酸化程度显著增加 (P<0.05)[3]

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

    分子量

    483.63

    Formula

    C28H29N5OS

    CAS 号
    性状

    固体

    颜色

    White to yellow

    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 27 mg/mL (55.83 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0677 mL 10.3385 mL 20.6770 mL
    5 mM 0.4135 mL 2.0677 mL 4.1354 mL
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    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

    • 方案 一

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

      Solubility: ≥ 2.5 mg/mL (5.17 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      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;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.17 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

      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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.57%

    参考文献
    Cell Assay
    [2]

    SH-SY5Y cells are transduced with 25% (v/v) BacMam LRRK2-GFP G2019S and plated (20 µL/well, 20,000 cells/well) onto eight 384-well assay plates. Then 25% BacMam LRRK2-GFP G2019S transduced SH-SY5Y cells are incubated with indicated concentrations of indicated compounds (e.g., IKK 16, 0.01, 0.1, 1, 10 and 100 μM) for 90 min prior to the TR-FRET detection with Tb-anti-LRRK2 pSer935 antibody. The % inhibition is calculated[2].

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

    Animal Administration
    [1][3]

    Rats and Mice[1]
    IKK 16 is tested in two animal models. First, its efficacy to inhibit TNFα release into plasma upon LPS-challenge in the rat is determined. IKK 16 is dosed sc (30 mg/kg) or orally (30 mg/kg) 1 h prior to the LPS-challenge. Four hours after the challenge, plasma is collected and the systemic TNFα levels are analyzed using a commercially available ELISA kit. Both routes of administration of IKK 16 at the indicated dose results in a significant inhibition of 86% (sc) and 75% (p.o.). In a second experiment, IKK 16 is also active in the thioglycollate-induced peritonitis model in the mouse. The maximal inhibition of neutrophil extravasation in this model is about 50% at a dose of 10 mg/kg sc.
    Mice[3]
    Two-month-old male C57BL/6 mice receive LPS (9 mg/kg body weight) and PepG (3 mg/kg body weight) in 0.9% saline (5 mL/kg body weight) intraperitoneally. Sham mice are not subjected to LPS/PepG, but are otherwise treated the same way. At 1 hour after LPS/PepG co-administration, mice are treated either with IKK 16 (1 mg/kg body weight i.v.) or vehicle (5 mL/kg body weight 10% DMSO i.v.). At 24 hours the experiment is terminated and organ and blood samples are collected for quantification of organ dysfunction and/or injury. Mice are randomly allocated into four different groups: (1) sham+vehicle (n=10); (2) sham+IKK 16 (n=3); (3) LPS/PepG+vehicle (n=9); (4) LPS/PepG+IKK 16 (n=10).

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

    参考文献

    IKK 16 相关分类

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0677 mL 10.3385 mL 20.6770 mL 51.6924 mL
    5 mM 0.4135 mL 2.0677 mL 4.1354 mL 10.3385 mL
    10 mM 0.2068 mL 1.0338 mL 2.0677 mL 5.1692 mL
    15 mM 0.1378 mL 0.6892 mL 1.3785 mL 3.4462 mL
    20 mM 0.1034 mL 0.5169 mL 1.0338 mL 2.5846 mL
    25 mM 0.0827 mL 0.4135 mL 0.8271 mL 2.0677 mL
    30 mM 0.0689 mL 0.3446 mL 0.6892 mL 1.7231 mL
    40 mM 0.0517 mL 0.2585 mL 0.5169 mL 1.2923 mL
    50 mM 0.0414 mL 0.2068 mL 0.4135 mL 1.0338 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    目录号:
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