1. Cell Cycle/DNA Damage
  2. IRE1
  3. MKC8866

MKC8866 

目录号: HY-104040 纯度: 98.76%
产品使用指南

MKC8866 是一种水杨醛类似物,有效的选择性 IRE1 RNase 抑制剂,在体外的 IC50 为 0.29 μM。 MKC8866 强烈抑制 Dithiothreitol 诱导的 XBP1s 表达,EC50 为 0.52 μM。MKC8866 抑制无应激 RPMI 8226 细胞,IC50 为 0.14 μM。 MKC8866 抑制乳腺癌细胞中的 IRE1 RNase 导致促肿瘤发生因子减少,同时也能抑制前列腺癌 (PCa) 肿瘤的生长。

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MKC8866 Chemical Structure

MKC8866 Chemical Structure

CAS No. : 1338934-59-0

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10 mM * 1 mL in DMSO ¥2640
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Top Publications Citing Use of Products

    MKC8866 purchased from MCE. Usage Cited in: Cancer Lett. 2020 Oct 10;490:76-88.

    RH30 and RD cells are treated with MKC8866 (20 μM) and/or AMGEN44 (2 μM) for 72 hours and Western blot confirmes IRE1 and PERK signalling inhibition. In cells treated with AMGEN44 alone or in combination with MKC8866, PERK phosphorylation is reduced and p-eIF2α protein levels are diminished. In cells treated with MKC8866 alone or in combination with AMGEN44, XBP1s protein levels are completely abolished.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MKC8866, a salicylaldehyde analog, is a potent, selective IRE1 RNase inhibitor with an IC50 of 0.29 μM in human vitro. MKC8866 strongly inhibits Dithiothreitol-induced X-box-binding protein 1-spliced (XBP1s) expression with an EC50 of 0.52 μM and unstresses RPMI 8226 cells with an IC50 of 0.14 μM[1]. MKC8866 inhibits IRE1 RNase in breast cancer cells leading to the decreased production of pro-tumorigenic factors and it can inhibits prostate cancer (PCa) tumor growth[2].

    IC50 & Target

    IC50: 0.29 μM (IRE1 RNase)[1]

    体外研究
    (In Vitro)

    MKC8866 (20 μM; 6 days) decreases proliferation of all breast cancer cell lines[2].
    MKC8866 (20 μM; 48 hours) reduces the number of cells entering S phase[2].
    MKC8866 (0.2-10 μM; 3 days) suppresses the viability of all four cell lines in a dose-dependent manner under normal conditions, with the most robust effect in LNCaP cells[1].
    MKC8866 (20 μM; 72 hours) is sufficient to completely block NSC 125973-induced expression of XBP1s [1].

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

    Cell Proliferation Assay[2]

    Cell Line: MCF7, SKBR3, MDA-MB-231 and MCF10A cells
    Concentration: 20 μM
    Incubation Time: For 6 days
    Result: Decreased proliferation of all breast cancer cell lines.

    Cell Cycle Analysis[2]

    Cell Line: MDA-MB-231, MCF7 and SKBR3 cells
    Concentration: 20 μM
    Incubation Time: 48 hours
    Result: Reduced the number of cells entering S phase.

    Cell Cycle Analysis[1]

    Cell Line: LNCaP, VCaP, 22Rv1 and C4-2B cells
    Concentration: 0.2, 0.5, 1, 5, 10 μM
    Incubation Time: 3 days
    Result: Suppressed the viability of all four cell lines in a dose-dependent manner.

    Cell Cycle Analysis[2]

    Cell Line: MDA-MB-231 cells
    Concentration: 20 μM
    Incubation Time: 72  hours
    Result: Completely blocked NSC 125973-induced expression of XBP1s.
    体内研究
    (In Vivo)

    MKC8866 (oral ; 300 mg/kg; for 28 days) reduces tumor regrowth post-NSC 125973 withdrawal[1].

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

    Animal Model: Female athymic nude mice with MDA-MB-231 tumor[1]
    Dosage: 300 mg/kg
    Administration: Oral; for 28 days
    Result: Reduced tumor regrowth post-NSC 125973 withdrawal.
    分子量

    361.35

    Formula

    C18H19NO7

    CAS 号
    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 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO : 16.67 mg/mL (46.13 mM; Need ultrasonic)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.7674 mL 13.8370 mL 27.6740 mL
    5 mM 0.5535 mL 2.7674 mL 5.5348 mL
    10 mM 0.2767 mL 1.3837 mL 2.7674 mL
    *

    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, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    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

    • 1.

      请依序添加每种溶剂: 10% DMSO    90% corn oil

      Solubility: ≥ 6.75 mg/mL (18.68 mM); Clear solution

      此方案可获得 ≥ 6.75 mg/mL (18.68 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

      以 1 mL 工作液为例,取 100 μL 67.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 2.

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

      Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

      此方案可获得 ≥ 1.67 mg/mL (4.62 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
    • 3.

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

      Solubility: ≥ 1.67 mg/mL (4.62 mM); Clear solution

      此方案可获得 ≥ 1.67 mg/mL (4.62 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 16.7 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。

      将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
    *以上所有助溶剂都可在 MCE 网站选购。
    参考文献

    纯度: 99.87%

    • 摩尔计算器

    • 稀释计算器

    The molarity calculator equation

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

    质量   浓度   体积   分子量 *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
    × = ×
    C1   V1   C2   V2

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    产品名称:
    MKC8866
    目录号:
    HY-104040
    需求量: