SKI V

CAS No. 24418-86-8

SKI V( —— )

Catalog No. M21983 CAS No. 24418-86-8

SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    SKI V
  • Note
    Research use only, not for human use.
  • Brief Description
    SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity
  • Description
    SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity.
  • In Vitro
    SKI V has weak activity toward ERK2 (IC50 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 IC50s 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 AnalysisCell Line:JC cells Concentration:0.2, 1, 5 μM Incubation Time:Pretreated for 1 hour Result:Decreased phospho-Akt and phospho-MEK levels.
  • In Vivo
    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 cellsDosage: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.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    S1P Receptor
  • Recptor
    SphK|PI3K
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    24418-86-8
  • Formula Weight
    254.24
  • Molecular Formula
    C15H10O4
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (196.66 mM)
  • SMILES
    Oc1ccc(\C=C2\Oc3ccccc3C2=O)cc1O
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.2. French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.
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