2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
- Product Name
- 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
- CAS No.
- 24418-86-8
- Chemical Name
- 2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V
- Synonyms
- SKI V;SKI V, 10 mM in DMSO;Sphingosine Kinase Inhibitor V;2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one;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;2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V;PI3K,SKI V,Inhibitor,Apoptosis,GST-hSK,sphingosine,second,mitogenic,Phosphoinositide 3-kinase,S1P,Sphingosine kinase,kinase,SphK,inhibit,antitumor,noncompetitive,messenger,non-lipid
- CBNumber
- CB22091422
- Molecular Formula
- C15H10O4
- Formula Weight
- 254.24
- MOL File
- 24418-86-8.mol
2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Property
- 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)
- pka
- 8.99±0.10(Predicted)
- form
- Solid
- color
- Light yellow to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P337+P313IF eye irritation persists: Get medical advice/attention.
N-Bromosuccinimide Price
- Product number
- CS-0012759
- Product name
- SKIV
- Purity
- 98.09%
- Packaging
- 5mg
- Price
- $280
- Updated
- 2021/12/16
- Product number
- CS-0012759
- Product name
- SKIV
- Purity
- 98.09%
- Packaging
- 10mg
- Price
- $450
- Updated
- 2021/12/16
- Product number
- CS-0012759
- Product name
- SKIV
- Purity
- 98.09%
- Packaging
- 50mg
- Price
- $1250
- Updated
- 2021/12/16
- Product number
- CS-0012759
- Product name
- SKIV
- Purity
- 98.09%
- Packaging
- 100mg
- Price
- $1850
- Updated
- 2021/12/16
- Product number
- 020427
- Product name
- SKIV
- Packaging
- 003
- Price
- $2100
- Updated
- 2021/12/16
2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one, Sphingosine Kinase Inhibitor V Chemical Properties,Usage,Production
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
Raw materials
Preparation Products
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