2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮

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

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)

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.