1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. HBX 19818

HBX 19818 是一种泛素蛋白特异性蛋白酶 (USP7) 抑制剂,IC50 值为 28.1 μM。

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HBX 19818 Chemical Structure

HBX 19818 Chemical Structure

CAS No. : 1426944-49-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2090
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2 mg ¥880
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5 mg ¥1900
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10 mg ¥3100
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50 mg ¥7300
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100 mg ¥9990
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Top Publications Citing Use of Products

    HBX 19818 purchased from MCE. Usage Cited in: Nat Chem Biol. 2017 Dec;13(12):1207-1215.  [Abstract]

    The effects of HBX19818 on FLT 3 expression in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment. The effects of P22077 on FLT 3 levels in FLT 3-ITD-expressing Ba/F3 cells after 22 h of treatment.

    HBX 19818 purchased from MCE. Usage Cited in: Mol Cell Biol. 2015 Apr 1;35(7):1157-68.  [Abstract]

    Western blot analysis of the chromatin fraction of HCT116 cells after treatment with the USP7 inhibitor HBX19818 for 4 or 8 h at 50 μM. Expression levels of USP7, RING1B, BMI1, and Ub-H2A are analyzed.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.

    IC50 & Target

    IC50: 28.1 μM (USP7)[1]

    体外研究
    (In Vitro)

    HBX 19818 是 USP7 的抑制剂,IC50 为 28.1 μM。HBX 19818 对 USP8、USP5、USP10、CYLD、UCH-L1、UCH-L3 或 SENP1 (一种 SUMO 蛋白酶) 没有影响,IC50 > 200 μM。HBX 19818 在人类癌细胞中选择性抑制 USP7,IC50 为 ~6 μM。此外,HBX 19818 (1.5、4、12、36 或 100 μM) 抑制多泛素化 p53 的 USP7 去泛素化。与 DMSO 处理的对照细胞相比,HBX 19818 (30 μM) 还在 USP7 过量生产的 HEK293 细胞中引起显著更高水平的 Mdm2 多泛素化形式。HBX 19818 以剂量依赖性方式抑制 HCT116 增殖,IC50 为 ~2 μM[1]

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

    分子量

    421.96

    Formula

    C25H28ClN3O

    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
    In Vitro: 

    1M HCl 中的溶解度 : 100 mg/mL (236.99 mM; 超声助溶; 酸性条件溶解 (HCL 调节,pH≈1))

    DMSO 中的溶解度 : 20 mg/mL (47.40 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 2.3699 mL 11.8495 mL 23.6989 mL
    5 mM 0.4740 mL 2.3699 mL 4.7398 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 mg/mL (4.74 mM); 澄清溶液

      此方案可获得 ≥ 2 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.0 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% Corn Oil

      Solubility: ≥ 2 mg/mL (4.74 mM); 澄清溶液

      此方案可获得 ≥ 2 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。

      1 mL 工作液为例,取 100 μL 20.0 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

    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: 99.35%

    参考文献
    Kinase Assay
    [1]

    The ability of HBX 19818 and HBX 28,258 to inhibit a panel of deubiquitinating enzymes, including UCH-L3 (13 pM), USP7 (100 pM), USP8 (1.36 nM), UCH-L1 (2.5 nM), USP5 (10 nM), USP20 (10 nM), and USP2 (500 pM), is tested using the UbAMC substrate (300 nM). The potential effects of HBX 19818 and HBX 28,258 are also tested on the enzymatic activities of SENP1 (80 pM), cathepsin-B (100 pM), and caspase-3 (100 pM) using the SUMO1-AMC (750 nM), ZRR-AMC (3 μM), and DEVD-AMC (250 nM) substrates, respectively. All enzymes are tested in USP7 reaction buffer (50 mM Tris-HCl [pH 7.6], 0.5 mM EDTA, 5 mM DTT, 0.01% Triton X-100, and 0.05 mg/mL serum albumin), except for two enzymes, USP8 (same buffer but pH 8.8) and caspase-3 (100 mM HEPES [pH 7.5], 10% sucrose, and 0.1% CHAPS). All enzymes are pre-incubated with DMSO or compounds (including HBX 19818) for 30 min at room temperature, and the enzymatic reaction is initiated by adding the substrate of interest. The reaction mixture is incubated at room temperature for 1 hr, and the reaction is stopped by adding acetic acid (100 mM). The reactions are monitored using the PHERAstar[1].

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

    Cell Assay
    [1]

    HCT116 cell proliferation is evaluated by incubating HCT116 cells for 30 min in culture medium containing 10 µM 5- bromo-2-deoxyuridine (BrdU), which is incorporated into the DNA of proliferating cells. Cells are then harvested by trypsin treatment, collected by centrifugation, and the pellet is resuspended and incubated in 70% ethanol for 30 min at 4°C. After centrifugation and supernatant removal, DNA is denaturated by incubating it in 2 N HCl for 30 min at room temperature. The percentage of BrdU-containing cells is then determined by flow cytometry, making it possible to quantify proliferating cells. Cell cycle is evaluated after treatment with HBX 19818 for 24 hr, followed by fixing detached cells and trypsinized cells in 70% ethanol for 30 minutes at 4°C. Cells are then incubated in PBS supplemented with 1% BSA, 0.5% Tween 20, 50 µg/mL RNase A and 50 µg/mL propidiumiodide for 30 minutes at 37°C. Samples are analyzed on a FACSort fluorocytometer. The percentage of cells in the different phases of the cell cycle is calculated using Multicycle software[1].

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

    参考文献

    HBX 19818 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 / 1M HCl 1 mM 2.3699 mL 11.8495 mL 23.6989 mL 59.2473 mL
    5 mM 0.4740 mL 2.3699 mL 4.7398 mL 11.8495 mL
    10 mM 0.2370 mL 1.1849 mL 2.3699 mL 5.9247 mL
    15 mM 0.1580 mL 0.7900 mL 1.5799 mL 3.9498 mL
    20 mM 0.1185 mL 0.5925 mL 1.1849 mL 2.9624 mL
    25 mM 0.0948 mL 0.4740 mL 0.9480 mL 2.3699 mL
    30 mM 0.0790 mL 0.3950 mL 0.7900 mL 1.9749 mL
    40 mM 0.0592 mL 0.2962 mL 0.5925 mL 1.4812 mL
    1M HCl 50 mM 0.0474 mL 0.2370 mL 0.4740 mL 1.1849 mL
    60 mM 0.0395 mL 0.1975 mL 0.3950 mL 0.9875 mL
    80 mM 0.0296 mL 0.1481 mL 0.2962 mL 0.7406 mL
    100 mM 0.0237 mL 0.1185 mL 0.2370 mL 0.5925 mL
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    • 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:
    HBX 19818
    目录号:
    HY-17540
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