SKI V

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SKI V

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

24418-86-8

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

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。

Cas No.	24418-86-8
别名	2-(3,4-二羟基亚苄基)苯并呋喃-3(2H)-酮
Canonical SMILES	O=C1/C(OC2=CC=CC=C12)=C/C3=CC=C(O)C(O)=C3
分子式	C₁₅H₁₀O₄
分子量	254.24
溶解度	DMSO: 250 mg/mL (983.32 mM)
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity[1][2]. SKI V has weak activity toward ERK2 (IC50 of 80 μM for hERK2) and does not inhibit PKC-α[1]. SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis[1]. 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[2]. SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ∼2 μM[1]. SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells[1].SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion[2]. Cell Proliferation Assay[1] Cell Line: T24 tumor cells SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals[1]. Animal Model: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells[1] [1]. French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9. [2]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.