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。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 K-7174 dihydrochloride 通常具有更好的水溶性和稳定性。

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K-7174 Chemical Structure

K-7174 Chemical Structure

CAS No. : 191089-59-5

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K-7174 的其他形式现货产品:

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
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献
    • 摩尔计算器

    • 稀释计算器

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    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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    目录号:
    HY-12743
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