2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
| 中文名称 | 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 |
|---|---|
| 中文同义词 | 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮;化合物SKI V |
| 英文名称 | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V |
| 英文同义词 | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V;SKI V;2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one;Sphingosine Kinase Inhibitor V;2-(3,4-Dihydroxybenzylidene)benzofuran-3(2H)-one;3(2H)-Benzofuranone, 2-[(3,4-dihydroxyphenyl)methylene]-;(2Z)-2-(3,4-dihydroxybenzylidene)-1-benzofuran-3(2H)-one;(2E)-2-[(3,4-dihydroxyphenyl)methylidene]-1-benzofuran-3-one |
| CAS号 | 24418-86-8 |
| 分子式 | C15H10O4 |
| 分子量 | 254.24 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 24418-86-8.mol |
| 结构式 |  |
2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 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 | 二甲基亚砜：250 mg/mL（983.32 mM） |
| 酸度系数(pKa) | 8.99±0.10(Predicted) |
IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)
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. |
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. |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-12895 | 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 SKI V | 24418-86-8 | 5mg | 2800元 |
| 2024/04/30 | HY-12895 | 2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮 SKI V | 24418-86-8 | 10mM * 1mLin DMSO | 3080元 |