2. NF-κB
  3. Keap1-Nrf2
  4. KI696

KI696 是一种干扰 Keap1/NRF2 相互作用的高亲和力探针。KI696 是有效、选择性的 KEAP1/NRF2 相互作用抑制剂。

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KI696 Chemical Structure

KI696 Chemical Structure

CAS No. : 1799974-70-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3028
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1 mg ￥1900
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5 mg ￥2500
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10 mg ￥4000
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25 mg ￥7600
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50 mg ￥9800
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200 mg   询价  

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Customer Review

Other Forms of KI696:

KI696 相关抗体

Top Publications Citing Use of Products

    KI696 purchased from MCE. Usage Cited in: Cell. 2019 Jul 11;178(2):330-345.e22.  [Abstract]

    Western blots showing levels of NRF2, NQO1, and BACH1 in mTC and mTN cells incubated for 24 hr with 5 μM KI-696 peptide to activate NRF2.

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    KI696 is a high affinity probe that disrupts the Keap1/NRF2 interaction. KI696 is a potent and selective inhibitor of the KEAP1/NRF2 interaction[1].

    IC50 & Target

    Target: Keap1-NRF2[1]
    体外研究
    (In Vitro)

    KI696 (compound 7) exhibits very high affinity for the KEAP1 Kelch domain (ITC Kd=1.3 nM with the exception of the organic anion transporting polypeptide 1B1 (OATP1B1) (IC50=2.5 µM), the bile salt export pump BSEP (IC50=4.0 µM), and the phosphodiesterase PDE3A (IC50=10 µM), no significant cross-reactivity is observed. No cytotoxicity is observed towards BEAS-2B cells with KI696 at concentrations up to 10 µM. KI696 increases NRF2 Nuclear Translocation in Normal Human Bronchial Epithelial cells. KI696 increases mRNA expression of the NRF2-dependent genes NQO1 and GCLM in NHBE cells transfected with the non-targeting siRNA, while NRF2 gene silencing significantly decreases compound activity. KI696 increases NQO1 Activity in an NRF2-Dependent Manner. Treatment with tBHP clearly has a detrimental effect on cell health and appearance while pre-treatment of cells with 1 µM KI696 before the exposure to tBHP maintained cell morphology consistent with the DMSO control. KI696 Induces the Expression of NRF2-Regulated Genes in COPD patient-derived bronchial epithelial cells[1].

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

    KI696 相关抗体:
    体内研究
    (In Vivo)

    KI696 induces the expression of each of the Nqo1, Ho-1, Txnrd1, Srxn1, Gsta3, Gclc genes in a dose-dependent manner, with maximum increases over vehicle controls of 37-(Nqo1), 17-(Ho-1), 9-(Txnrd1), 28-(Srxn1), 15-(Gsta3) and 13-fold (Gclc) occurring at the 50 µmol/kg dose. EC50 values are 44.0, 25.7, 42.6, 33.8, 28.4, and 44.1 µmol/kg, respectively, giving an average EC50 value of 36.4±3.4 µmol/kg. KI696 attenuates ozone-Induced pulmonary inflammation. KI696 restores ozone-induced depletion of lung GSH levels. KI696 is administered to rats at 10, 35 and 50 µmol/kg by IV infusion, resulting in steady state compound concentrations in the blood of 407±44 nM, 946±50 nM and 1437±186 nM, respectively, over the 6 hour infusion period. Exposure to ozone 24 hours post-dose produces a significant depletion in lung levels of the anti-oxidant molecule, GSH, which is restored by KI696 in a dose-dependent manner[1].

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

    550.63

    Formula

    C28H30N4O6S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 : 50 mg/mL (90.81 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 1.8161 mL 9.0805 mL 18.1610 mL
    5 mM 0.3632 mL 1.8161 mL 3.6322 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.5 mg/mL (4.54 mM); 悬浊液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.78 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

      以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

    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: 99.26%

    COA (194 KB) HNMR (150 KB) RP-HPLC (100 KB) LCMS (337 KB)

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

    Inhibition of the Kelch domain-NRF2 interaction is determined using a fluorescence polarisation-based competition assay in a black 384-well microplate. Each well contained 2 nM 5’-TAMRA-NRF2 peptide (AFFAQLQLDEETGEFL) and 7 nM human KEAP1 (residues 321-609) in 50 µL of assay buffer (50 mM Tris-HCl pH 8.0, 100 mM NaCl, 5 mM MgCl2, 2 mM 3-[(3-Cholamidopropyl)dimethylammonio]-1-propanesulfonate (CHAPS), 1 mM DTT, 0.005% BSA, 1% DMSO). After 1 hour at room temperature, fluorescence polarisation (excitation 485 nm/emission 520 nm) is measured using a BMG Pherastar FS plate reader. IC50 values are determined by fitting the data to a four parameter logistic fit[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    BEAS-2B cells are plated in 384 well black clear-bottomed plates and are incubated overnight (37°C, 5% CO2). On day 2, the plates are centrifuged and 50 nL of compound (KI696) or controls are added to the cells for 48 hours. On day 4, the medium is aspirated from the plate and crude cell lysates are made by using 1X lysis buffer with Complete, Mini, EDTA-free Protease Inhibitor. After lysis, the plates are incubated for 20 minutes at room temperature and the MTT cocktail is prepared for measurement of NQO1 activity. The samples are analyzed on an Envision plate reader, reading absorbance at 570 nm for five individual readings with 10 minute intervals. Product formation is measured kinetically and the pEC50 of NQO1 specific activity induction is calculated by plotting the change in absorbance versus log [compound] followed by 4-parameter fitting[1].

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

    Rats[1]

    To examine the effect of KI696 under conditions of oxidative stress, rats are administered KI696 at 35 µmol/kg (the approximate average EC50 value for gene expression) by IV infusion over 6 hours, and after 24 hours are exposed to ozone (1 ppm for 3 hours). Fifteen minutes following the termination of ozone exposure, the numbers of total cells, neutrophils and mononuclear cells in the bronchoalveolar lavage (BAL) fluid are measured[1].

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

    KI696 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 1.8161 mL 9.0805 mL 18.1610 mL 45.4025 mL
    5 mM 0.3632 mL 1.8161 mL 3.6322 mL 9.0805 mL
    10 mM 0.1816 mL 0.9081 mL 1.8161 mL 4.5403 mL
    15 mM 0.1211 mL 0.6054 mL 1.2107 mL 3.0268 mL
    20 mM 0.0908 mL 0.4540 mL 0.9081 mL 2.2701 mL
    25 mM 0.0726 mL 0.3632 mL 0.7264 mL 1.8161 mL
    30 mM 0.0605 mL 0.3027 mL 0.6054 mL 1.5134 mL
    40 mM 0.0454 mL 0.2270 mL 0.4540 mL 1.1351 mL
    50 mM 0.0363 mL 0.1816 mL 0.3632 mL 0.9081 mL
    60 mM 0.0303 mL 0.1513 mL 0.3027 mL 0.7567 mL
    80 mM 0.0227 mL 0.1135 mL 0.2270 mL 0.5675 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:

    KI6961799974-70-1KI 696KI-696Keap1-Nrf2Inhibitorinhibitorinhibit

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