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Shanghai YuanYe Biotechnology Co., Ltd.
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Product Name:2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
CAS:24418-86-8
Purity:98% Package:1mg Remarks:Y69232
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| | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Basic information |
| Product Name: | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V | | Synonyms: | 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;(2E)-2-[(3,4-dihydroxyphenyl)methylidene]-1-benzofuran-3-one;(2Z)-2-(3,4-dihydroxybenzylidene)-1-benzofuran-3(2H)-one;3(2H)-Benzofuranone, 2-[(3,4-dihydroxyphenyl)methylene]-;2-(3,4-Dihydroxybenzylidene)benzofuran-3(2H)-one | | CAS: | 24418-86-8 | | MF: | C15H10O4 | | MW: | 254.24 | | EINECS: | | | Product Categories: | | | Mol File: | 24418-86-8.mol |  |
| | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Chemical Properties |
| Boiling point | 493.2±45.0 °C(Predicted) | | density | 1.489±0.06 g/cm3(Predicted) | | storage temp. | Sealed in dry,2-8°C | | solubility | DMSO: 250 mg/mL (983.32 mM) | | form | Solid | | pka | 8.99±0.10(Predicted) | | color | Light yellow to yellow |
| | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Usage And Synthesis |
| Uses | 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]. | | Definition | ChEBI: 3',4'-dihydroxyaurone is a hydroxyaurone that is aurone which is substituted by hydroxy groups at the 3' and 4' positions; major species at pH 7.3. It shows inhibitory activity against several isoforms of the histone deacetylase complex (HDAC). It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a hydroxyaurone and a member of catechols. It is functionally related to a 2',3,4-trihydroxy-trans-chalcone. | | Biological Activity | SKI V is a non-competitive, potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with IC50 of 2 μM against GST-hSK. SKI V potently inhibits PI3K with IC50 of 6 μM for hPI3k. SKI V reduces the formation of the mitotic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity. | | in vivo | SKI V (75 mg/kg; ip; 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: | < td class="col2"> IP; days 1, 5, 9, 15 | Result: | Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals. | | | target | IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2) | | References | [1] French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9. PMID:14522923
[2] French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603. DOI:10.1124/jpet.106.101345 |
| | 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Preparation Products And Raw materials |
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