2. NF-κB
  3. IKK
  4. SC-514

SC-514  (Synonyms: GK 01140)

目录号: HY-13802 纯度: 99.89%
COA 产品使用指南

摩尔计算器

SC-514 是一种选择性 IKK-2 抑制剂 (IC50=11.2 μM)，不抑制其他 IKK 亚型或其他丝氨酸-苏氨酸和酪氨酸激酶。

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SC-514 Chemical Structure

SC-514 Chemical Structure

CAS No. : 354812-17-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥335
In-stock
5 mg ￥300
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10 mg ￥550
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50 mg ￥1300
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100 mg ￥2000
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

SC-514 相关抗体

Top Publications Citing Use of Products

    SC-514 purchased from MCE. Usage Cited in: Dig Dis Sci. 2019 May;64(5):1204-1216.  [Abstract]

    The expression of BAX, Bcl2, P53, PARP, cleaved caspase 3, and cleaved caspase 9 in SGC-7901 cells is measured by western blotting in the treatment of SC-514.

    查看 IKK 亚型特异性产品:

    查看所有亚型
    IKK-α IKK-β IKK IKKε TBK1

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SC-514 is a selective IKK-2 inhibitor (IC50=11.2 μM), which does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.

    IC50 & Target[1]

    IKK-2

    11.2 μM (IC50)

    CDK2/A

    61 μM (IC50)

    AUR2

    71 μM (IC50)

    PRAK

    75 μM (IC50)

    MSK

    123 μM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    NIH3T3 IC50
    7.9 μM
    Compound: SC415
    Inhibition of TNFalpha-induced NFkappaB activation in mouse NIH-3T3 cells expressing NFkappaB (unknown origin) preincubated for 15 mins followed by TNFalpha addition measured after 6 hrs by luciferase reporter gene assay
    Inhibition of TNFalpha-induced NFkappaB activation in mouse NIH-3T3 cells expressing NFkappaB (unknown origin) preincubated for 15 mins followed by TNFalpha addition measured after 6 hrs by luciferase reporter gene assay
    		[PMID: 27352042]
    体外研究
    (In Vitro)

    SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer with IC50s of 6.1±2.2 μM and 2.7±0.7 μM, respectively. IKK-2 inhibition by SC-514 is selective, reversible, and competitive with ATP. SC-514 inhibits transcription of NF-κB-dependent genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts in a dose-dependent manner. SC-514 inhibits all forms of recombinant human IKK-2 including rhIKK-2 homodimer, rhIKK-1/rhIKK-2 heterodimer, as well as the constitutively active form of rhIKK-2 with comparable IC50 values in the 3-12 μM range[1]. To evaluate whether the reactive oxygen species (ROS)-inducing IKKβ inhibitor increases the sensitivity of melanoma cells to nitrosourea. The responses of melanoma cells are first assessed to SC-514/Fotemustine co-treatment. Melanoma cell lines are treated with 50 µM of SC-514 and Fotemustine alone and in combination for 48 h and growth inhibition is assessed. Co-treatment with SC-514 significantly enhances Fotemustine-induced cytotoxicity in all melanoma cell lines tested[2].

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

    SC-514 相关抗体:
    体内研究
    (In Vivo)

    SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNFα production in the rat. SC-514 shows a dose-dependent inhibition of TNFα production, validating IKK-2 as a potential anti-inflammatory drug target in vivo[1]. To obtain in vivo evidence for the implication of SC-514 in the response of cancer cells to Fotemustine, the xenograft mouse model of melanoma is used. Nude mice engrafted with A375 or G361 tumors are treated with vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days and the tumor behavior is monitored. Fotemustine treatment with SC-514 shows a clear combined effect and reduces the size of tumors in mice[2].

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

    224.30

    Formula

    C9H8N2OS2
    CAS 号
    性状

    固体

    颜色

    Light yellow 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
    细胞实验： 

    DMSO 中的溶解度 : 50 mg/mL (222.92 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 4.4583 mL 22.2916 mL 44.5831 mL
    5 mM 0.8917 mL 4.4583 mL 8.9166 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

    动物实验：

    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 (11.15 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。

      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；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 (11.15 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。

      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 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      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

    只
    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: 99.89%

    COA (287 KB) LCMS (95 KB)

    产品使用指南 (1538 KB)
    参考文献
    Kinase Assay
    [1]

    IKK complexes are immunoprecipitated from IL-1β-treated RASF cell lysates (0.5-2 mg) using a NEMO antibody (3-10 μg) followed by the addition of protein A-agarose beads. Antibody complexes are pelleted by centrifugation and washed 3 times with 1 mL of cold whole-cell lysis buffer followed by 2 washes in kinase buffer (25 mM HEPES, pH 7.6, 2 mM MgCl2, 2 mM MnCl2, 10 mM NaF, 5 mM DTT, and 1 mM phenylmethylsulfonyl fluoride). 100-200 μg of immunoprecipitated IKK is analyzed for kinase activity in a reaction containing 10 μM biotinylated IκBα peptide as substrate and 1 μM [γ-33P]ATP (2500 Ci/mmol). After incubation at room temperature for 30 min, 25 μL of the reaction mixture is withdrawn and added to a SAM 96 biotin capture plate. After successive wash steps the plate was allowed to air-dry, and 25 μL of scintillation fluid is added to each well. Incorporation of [γ-33P]ATP is measured using a Top-Count NXT[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    For crystal violet staining assay, melanoma cell lines (1×104) are seeded in 60 mm dishes, and then untreated or pretreated with SC-514 (50 µM) and/or Fotemustine. Then, cells are formalin-fixed and stained with crystal violet. Cell numbers are measured as the optical density at 595 nm (OD595) of solubilized crystal violet from formalin-fixed cells. Cytotoxicity are also determined by the MTT reduction assay[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][2]

    Rats[1]
    SC-514 or vehicle (2% Me2SO in saline) is administered either by oral gavage (50 mg/kg) or intraperitoneally (10 and 50 mg/kg) to adult male Wistar rats that have been deprived of food overnight. Two hours after compound treatment, 1 mg/kg LPS (Escherichia coli) in saline is administered intraperitoneally 90 min after LPS administration; the animals are bled and serum TNFα levels analyzed by a rat-specific TNFα ELISA.
    Mice[2]
    Male nu/nu BALB/c mice (6 weeks old) are maintained in individual ventilated cages. A375 or G361 (5×106) cells are resuspended in 0.1 mL PBS and inoculated subcutaneously into the backs of nude mice and allowed to grow for 7 days. After that, mice are randomly assigned to 4 groups (n=6 for each group) and treated by intraperitoneal injection with 200 µL 30% PEG/5% Tween-80 solution as the vehicle control and 25 mg/kg SC-514 and/or 25 mg/kg Fotemustine daily for 13-15 consecutive days. Body weight and tumor volume are measured every 3 days. Tumor volumes are determined by a caliper and calculated. At the end of the experiment, mice are sacrificed and tumor xenografts are collected. Tumor tissues are stored at -80°C for Western blot analysis.

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

    SC-514 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 4.4583 mL 22.2916 mL 44.5831 mL 111.4579 mL
    5 mM 0.8917 mL 4.4583 mL 8.9166 mL 22.2916 mL
    10 mM 0.4458 mL 2.2292 mL 4.4583 mL 11.1458 mL
    15 mM 0.2972 mL 1.4861 mL 2.9722 mL 7.4305 mL
    20 mM 0.2229 mL 1.1146 mL 2.2292 mL 5.5729 mL
    25 mM 0.1783 mL 0.8917 mL 1.7833 mL 4.4583 mL
    30 mM 0.1486 mL 0.7431 mL 1.4861 mL 3.7153 mL
    40 mM 0.1115 mL 0.5573 mL 1.1146 mL 2.7864 mL
    50 mM 0.0892 mL 0.4458 mL 0.8917 mL 2.2292 mL
    60 mM 0.0743 mL 0.3715 mL 0.7431 mL 1.8576 mL
    80 mM 0.0557 mL 0.2786 mL 0.5573 mL 1.3932 mL
    100 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1146 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.

    Keywords:

    SC-514354812-17-2GK 01140SC514SC 514GK01140GK-01140IKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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