Ceranib-2 |
カタログ番号GC15981 |
セラニブ-2 は、SKOV3 細胞で 28 μM の IC50 で細胞のセラミダーゼ活性を阻害する強力な非脂質性セラミダーゼ阻害剤です。セラニブ 2 は、複数のセラミド種の蓄積を誘導し、スフィンゴシンとスフィンゴシン-1-リン酸 (S1P) のレベルを低下させ、細胞アポトーシスを誘導します。抗がん作用。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1402830-75-4
Sample solution is provided at 25 µL, 10mM.
IC50: 28 μM
Ceranib-2 is an inhibitor of cellular ceramidase activity.
Ceramidase catalyzes the hydrolysis of the N-acyl linkage between the fatty acid and sphingosine base in ceramide to produce sphingosine and a free fatty acid. Ceramidase plays a key role in regulating cell fate and its inhibition in both malignant and non-cancerous cells results in apoptosis.
In vitro: In a previous study, a more potent analogue (Ceranib-2) of novel ceramidase inhibitor (Ceranib-1) was identified by screening a small molecule library. In a cell-based assay, both Ceranib-1 and Ceranib-2 were able to inhibit cellular ceramidase activity, decrease levels of sphingosine and S1P, inhibit the proliferation of cells alone and, induce the accumulation of multiple ceramide species, and induce cell-cycle arrest and death in combination with paclitaxel [1].
In vivo: In a previous study, Ceranib-2 was given by i.p. injection on 5 days per week. Resutls showed that the average normalized size of tumors in each treatment group increased over time. However, by day 11 Ceranib-2-treated groups had significantly lower tumor volumes. By day 21, the average normalized tumor volumes for the control, 20 mg/kg and 50 mg/kg Ceranib-2 groups were 1,400, 940, and 710, respectively. In addition, the administration of Ceranib-2 did not alter the total body weight of the mice [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Draper, J. M.,Xia, Z.,Smith, R.A., et al. Discovery and evaluation of inhibitors of human ceramidase. Molecular Cancer Therapeutics 1-27 (2011).
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