1. Metabolic Enzyme/Protease Apoptosis
  2. Proteasome Apoptosis
  3. K-7174

K-7174 是具有口服活性的 proteasomeGATA 的抑制剂。K-7174 抑制细胞黏附。K-7174 诱导细胞凋亡。K-7174 具有抗肿瘤活性,可用于癌症的研究。

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K-7174 Chemical Structure

K-7174 Chemical Structure

CAS No. : 191089-59-5

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Other Forms of K-7174:

    K-7174 purchased from MCE. Usage Cited in: Brain Res. 2022.

    K-7174 (30 mg/kg; i.p.; 3 times a week for 6 weeks) improves lupus-like symptoms in MRL/lpr mice. The deposition of IgG and C3 in the kidneys of mice in the MRL/lpr group is significantly higher than that in the control group, but K-7174 can significantly inhibit this deposition.

    K-7174 purchased from MCE. Usage Cited in: Brain Res. 2022.

    K-7174 significantly increases the protein and gene levels of ZO1 and Occludin in NPSLE model mouse (MRL/lpr mice) brain.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer[1][2][3].

    体外研究
    (In Vitro)

    K-7174 (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand[1].
    K-7174 (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM[1].
    K-7174 (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM[1].
    K-7174 (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells[2].
    K-7174 (2.5-30 μM; 24 h) inhibits the binding activity of GATA[2].
    K-7174 (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis[3].

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

    Cell Viability Assay[3]

    Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
    Concentration: 0-25 μM
    Incubation Time: 72 h
    Result: Inhibited MM cells growth.

    Apoptosis Analysis[3]

    Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
    Concentration: 10 μM
    Incubation Time: 48 h
    Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.
    体内研究
    (In Vivo)

    K-7174 (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].
    K-7174 (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo[3].
    K-7174 (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection[3].

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

    Animal Model: ICR mice with IL-β or TNF-α injection[2]
    Dosage: 30 mg/kg
    Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days
    Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations
    Animal Model: NOD/SCID mice with murine xenograft[3]
    Dosage: 75 mg/kg
    Administration: Intraperitoneal injection; once daily for 14 days
    Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
    Animal Model: NOD/SCID mice with murine xenograft[3]
    Dosage: 50 mg/kg
    Administration: Oral gavage; once daily for 14 days
    Result: Showed an anti-myeloma activity. Proved oral administration is more effective than intraperitoneal injection.
    分子量

    568.74

    Formula

    C33H48N2O6

    CAS 号
    性状

    油状物

    颜色

    Colorless to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Pure form -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (175.83 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 1.7583 mL 8.7914 mL 17.5827 mL
    5 mM 0.3517 mL 1.7583 mL 3.5165 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, 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。

    • 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: ≥ 5 mg/mL (8.79 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 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: ≥ 5 mg/mL (8.79 mM); 澄清溶液

      此方案可获得 ≥ 5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 50.0 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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

    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
    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, 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7583 mL 8.7914 mL 17.5827 mL 43.9568 mL
    5 mM 0.3517 mL 1.7583 mL 3.5165 mL 8.7914 mL
    10 mM 0.1758 mL 0.8791 mL 1.7583 mL 4.3957 mL
    15 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9305 mL
    20 mM 0.0879 mL 0.4396 mL 0.8791 mL 2.1978 mL
    25 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
    30 mM 0.0586 mL 0.2930 mL 0.5861 mL 1.4652 mL
    40 mM 0.0440 mL 0.2198 mL 0.4396 mL 1.0989 mL
    50 mM 0.0352 mL 0.1758 mL 0.3517 mL 0.8791 mL
    60 mM 0.0293 mL 0.1465 mL 0.2930 mL 0.7326 mL
    80 mM 0.0220 mL 0.1099 mL 0.2198 mL 0.5495 mL
    100 mM 0.0176 mL 0.0879 mL 0.1758 mL 0.4396 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:
    K-7174
    目录号:
    HY-12743
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