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
- 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.
- 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
- 公司名称：Aladdin Scientific
- 联系电话：+1-+1(833)-552-7181
- 电子邮件：sales@aladdinsci.com
- 国家：美国
- 产品数：57505
- 优势度：58
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：
- 电子邮件：support@targetmol.com
- 国家：美国
- 产品数：38631
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
- 公司名称：SIGMAALDRICH
- 联系电话：--
- 电子邮件：
- 国家：美国
- 产品数：6773
- 优势度：87
