1. Immunology/Inflammation Apoptosis
  2. SphK Apoptosis
  3. K145

K145 是一种选择性的,具有底物竞争性和口服活性的 SphK2 抑制剂,IC50 为 4.3 µM,Ki 为 6.4 µM。K145 对 SphK1 和其他蛋白激酶没有活性。K145 可诱导细胞凋亡,并具有强大的抗肿瘤活性。

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K145 Chemical Structure

K145 Chemical Structure

CAS No. : 1309444-75-4

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Top Publications Citing Use of Products

    K145 purchased from MCE. Usage Cited in: Am J Cancer Res. 2019 Mar 1;9(3):546-561.  [Abstract]

    Western immunoblotting analysis of NOXA protein levels in RBE and HCCC9810 cells treated with different concentrations of K145 for 24 h. Data shown represents 2 independent experiments.

    K145 purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2017 Nov 4;493(1):286-290.  [Abstract]

    Inhibition of pAkt by API-2 effectively prevents K145 induced increasing phosphorylation of FoxO1 in response to insulin. API-2 also significantly reverses K145 suppressed PEPCK and G6Pase mRNA and protein expression.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity[1].

    IC50 & Target

    IC50: 4.3 µM (SphK2)[1]
    Ki: 6.4 µM (SphK2)[1]

    体外研究
    (In Vitro)

    K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner[1].
    K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells[1].
    K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt[1].
    Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels[1].

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

    Cell Viability Assay[1]

    Cell Line: U937 cells
    Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM
    Incubation Time: 24 hours, 48 hours, 72 hours
    Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

    Apoptosis Analysis[1]

    Cell Line: U937 cells
    Concentration: 10 µM
    Incubation Time: 24 hours
    Result: Significantly induced apoptosis in U937 cells.

    Western Blot Analysis[1]

    Cell Line: U937 cells
    Concentration: 4 µM, 8 µM
    Incubation Time: 3 hours
    Result: Phosphorylated ERK and Akt were decreased.
    体内研究
    (In Vivo)

    K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice[1].

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

    Animal Model: BALB/c-nu mice injected with U937 cells[1]
    Dosage: 50 mg/kg
    Administration: Oral gavage; daily; for 15 days
    Result: Oral gavage; daily; for 15 daysInhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
    分子量

    348.46

    Formula

    C18H24N2O3S

    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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    产品名称:
    K145
    目录号:
    HY-15779
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