1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. KRIBB11

KRIBB11 是 HSF1 的抑制剂,IC50 值为 1.2 μM。

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KRIBB11 Chemical Structure

KRIBB11 Chemical Structure

CAS No. : 342639-96-7

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605
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1 mg ¥250
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5 mg ¥550
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10 mg ¥800
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25 mg ¥1613
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50 mg ¥3000
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100 mg ¥4600
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200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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Top Publications Citing Use of Products

    KRIBB11 purchased from MCE. Usage Cited in: Arch Biochem Biophys. 2023 Jan 23;109525.  [Abstract]

    KRIBB11 (0, 10, 20 µM; 24 h)completely blocks n-butyrate-mediated HSP70 expression and Hspa1α promoter activation in Caco-2 cells (fig B and C).

    KRIBB11 purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Dec 12;8(12):3203.  [Abstract]

    Immunoblot showing that HSF1 inhibitor KRIBB11 and transcription inhibitor Act-D both fail to block RIP140 degradation.

    KRIBB11 purchased from MCE. Usage Cited in: Mol Oncol. 2017 Oct;11(10):1475-1492.  [Abstract]

    (A) IHC staining of N-cadherin and E-cadherin in the pancreas from KPC mice treated with vehicle, Metformin, or KRIBB11. (B) Masson's trichrome staining and IHC staining of α-SMA in pancreatic tissues from mice treated with vehicle, Metformin, or KRIBB11.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    KRIBB11 is an inhibitor of Heat shock factor 1 (HSF1), with IC50 of 1.2 μM.

    IC50 & Target[1]

    HSF1

    1.2 μM (IC50)

    体外研究
    (In Vitro)

    KRIBB11 阻断 HSP27 和 HSP70HSF1 下游靶蛋白的诱导。KRIBB11 诱导 HCT-116 细胞的生长停滞和细胞凋亡。KRIBB11 抑制依赖于 HSF1 的 p-TEFb(正转录延伸因子 b)募集到 hsp70 启动子[1]。在用 KRIBB11 处理的细胞中,PARPcaspase-3 裂解增加。 用 KRIBB11 孵育 RKO,毒性阈值约为 10 μM,IC50 为 20-30 μM[2]

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

    体内研究
    (In Vivo)

    KRIBB11 (50 mg/kg,腹腔注射) 抑制裸鼠体内 47.4% 的肿瘤生长,体重没有减轻[1]

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

    分子量

    284.27

    Formula

    C13H12N6O2

    CAS 号
    性状

    固体

    颜色

    Yellow to orange

    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 : 125 mg/mL (439.72 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 3.5178 mL 17.5889 mL 35.1778 mL
    5 mM 0.7036 mL 3.5178 mL 7.0356 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 (8.79 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。
    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: 99.54%

    参考文献
    Kinase Assay
    [1]

    HCT-116 cells are washed with PBS and then homogenized with a 27-gauge syringe in binding buffer (10 mm Tris-HCl (pH 7.4), 50 mm KCl, 5 mm MgCl2, 1 mm EDTA, and 0.1 mm Na3VO4). The cell lysate is centrifuged at 13,000 rpm for 30 min at 4°C, and the supernatant is collected. The HCT-116 cell lysate supernatant is precleared by incubating with Dynabeads M-280 streptavidin for 30 min at 4°C and captured by magnet separation. The cleared supernatants are incubated with biotinyl-KRIBB11 compound. After overnight incubation at 4°C, proteins associated with the biotinyl-KRIBB11 compound are precipitated with Dynabeads M-280 streptavidin. Precipitated samples are separated by a magnet. Samples are washed with 1 mL of ishing buffer containing 50 mm HEPES (pH 7.5), 50 mm NaCl, 1 mm EDTA, 1 mm EGTA, 0.1% Tween 20, 10% (v/v) glycerol, 1 mm NaF, 0.1 mm Na3VO4, and protease inhibitor mixture tablets (1 tablet/10 mL). Samples are boiled in SDS-PAGE sample buffer, separated by 10% polyacrylamide gel, and immunoblotted with antibodies against HSF1, HSF2, HSP90, or CDK9.

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

    Cell Assay
    [1]

    Cells are seeded onto 96-well plates at a density of 6×103 cells per well in McCoy's 5A medium with 10% FBS. After 24 h, the medium is replenwashed with fresh complete medium containing chemicals or 0.1% DMSO. After incubation for 48 h, the cell proliferation reagent WST-1 is added to each well. The amount of WST-1 formazan produced is measured at 450 nm using an ELISA reader.

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

    Animal Administration
    [1]

    Seven-week-old female inbred specific pathogen-free Balb/c nude mice are housed under sterile conditions with 12-h light/dark cycles, and fed food and water ad libitum. For the evaluation of the in vivo anti-tumor activity of KRIBB11, HCT-116 cells (0.3 mL of 4×107 cells/mL) are implanted subcutaneously into the right flank of the mice on day 0. KRIBB11 is dissolved in 10% dimethylacetamide, 50% PEG300, and 40% distilled water. When the size of tumors reached 72.2 mm3, the compound is administered intraperitoneally at a dose of 50 mg/kg/day for 18 days. Tumor volumes are estimated by using the formula length (mm) × width (mm) × height (mm)/2. To determine the toxicity of the compound, the body weight of tumor-bearing animals is recorded. On day 18, the mice are sacrificed, and the tumors are weighed.

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

    参考文献

    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 3.5178 mL 17.5889 mL 35.1778 mL 87.9446 mL
    5 mM 0.7036 mL 3.5178 mL 7.0356 mL 17.5889 mL
    10 mM 0.3518 mL 1.7589 mL 3.5178 mL 8.7945 mL
    15 mM 0.2345 mL 1.1726 mL 2.3452 mL 5.8630 mL
    20 mM 0.1759 mL 0.8794 mL 1.7589 mL 4.3972 mL
    25 mM 0.1407 mL 0.7036 mL 1.4071 mL 3.5178 mL
    30 mM 0.1173 mL 0.5863 mL 1.1726 mL 2.9315 mL
    40 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1986 mL
    50 mM 0.0704 mL 0.3518 mL 0.7036 mL 1.7589 mL
    60 mM 0.0586 mL 0.2931 mL 0.5863 mL 1.4657 mL
    80 mM 0.0440 mL 0.2199 mL 0.4397 mL 1.0993 mL
    100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.8794 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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    产品名称:
    KRIBB11
    目录号:
    HY-100872
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