生物活性 靶点 体外研究 体内研究 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 试剂级价格
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2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮

2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮,24418-86-8,结构式
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
  • CAS号:24418-86-8
  • 英文名:2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
  • 中文名:2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
  • CBNumber:CB22091422
  • 分子式:C15H10O4
  • 分子量:254.24
  • MOL File:24418-86-8.mol
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮化学性质
  • 沸点 :493.2±45.0 °C(Predicted)
  • 密度 :1.489±0.06 g/cm3(Predicted)
  • 储存条件 :Sealed in dry,2-8°C
  • 溶解度 :DMSO: 250 mg/mL (983.32 mM)
  • 酸度系数(pKa) :8.99±0.10(Predicted)
  • 形态 :Solid
  • 颜色 :Light yellow to yellow

2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮性质、用途与生产工艺

  • 生物活性 SKI V 是一种非竞争性的,有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂,对 GST-hSK 的 IC50 为 2 μM。 SKI V 有效抑制 PI3K,对 hPI3k 的 IC50 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。
  • 靶点

    IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)

  • 体外研究

    SKI V has weak activity toward ERK2 ( IC 50 of 80 μM for hERK2) and does not inhibit PKC-α.
    SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis.
    SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour.
    SKI V has IC 50 s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM.
    SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.
    SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion.

    Cell Proliferation Assay

    Cell Line: T24 tumor cells
    Concentration: 10 μM
    Incubation Time: For 24 hours
    Result: Inhibited cancer cell proliferation.

    Apoptosis Analysis

    Cell Line: T24 tumor cells
    Concentration: 10 μM
    Incubation Time: For 24 hours
    Result: Induced apoptosis.

    Western Blot Analysis

    Cell Line: JC cells
    Concentration: 0.2, 1, 5 μM
    Incubation Time: Pretreated for 1 hour
    Result: Decreased phospho-Akt and phospho-MEK levels.
  • 体内研究

    SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.

    Animal Model: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells
    Dosage: 75 mg/kg
    Administration: IP; days 1, 5, 9, 15
    Result: Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.
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2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 试剂级价格
  • 更新日期:2024/11/08
  • 产品编号:HY-12895
  • 产品名称:2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 SKI V
  • CAS编号:24418-86-8
  • 包装:5mg
  • 价格:1500元
  • 更新日期:2024/11/08
  • 产品编号:HY-12895
  • 产品名称:2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 SKI V
  • CAS编号:24418-86-8
  • 包装:10mM * 1mLin DMSO
  • 价格:1650元
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮生产厂家
  • 公司名称:SIGMA
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  • 国家:瑞士
  • 产品数:6896
  • 优势度:91