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

K145 

目录号: HY-15779
产品使用指南

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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K145 的其他形式现货产品:

Other Forms of K145:

Top Publications Citing Use of Products

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

    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.

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

    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.
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    Description

    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]

    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].

    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.
    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].

    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.
    Molecular Weight

    348.46

    Formula

    C₁₈H₂₄N₂O₃S

    CAS No.

    1309444-75-4

    SMILES

    O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

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

    References
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    The molarity calculator equation

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    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    K145K 145K-145SPHKApoptosisSphingosine kinaseSphK2S1PERKAktapoptoticsubstrate-competitivesphingosineantitumororalanti-proliferativeInhibitorinhibitorinhibit

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    目录号:
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