NVP 231  ≥98%

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包装规格:10mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(≥ 100 mg/mL)
产品描述:基本信息 产品编号:N10625 产品名称:NVP 231 CAS: 362003-83-6   储存条件 粉末 -20℃ 四年     分子式: C25H25N3O2S 溶于液体 -80℃ 六个月 分子量 431.55 -20℃ 一个月 化学名:      Solubility (25°C)   体外 DMSO 86mg/mL (199.28mM) Ethanol 8mg/mL (18.53mM) Water Insoluble 体内(现配现用)     <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.3172mL 11.5861mL 23.1723mL 5mM 0.4634mL 2.3172mL 4.6345mL 10mM 0.2317mL 1.1586mL 2.3172mL 50mM 0.0463mL 0.2317mL 0.4634mL   生物活性 产品描述 一种强效、特异、可逆的神经酰胺激酶 (CerK) 抑制剂 (IC50=12nM),可竞争性地抑制神经酰胺与 CerK 的结合。 靶点/IC50 12nM (CerK); apoptosis   体外研究 NVP-231 (0-500 nM; 24 hours) gradually reduces the cellular CerK activity, as measured by NBD-C1P formation,demonstrating that NVP-231 active in transfected cells. The IC50 for CerK in this cellular system is 59.70 ± 12nM.NVP-231 (0-1000nM; 48 hours) decreases cell viability as a dose-dependent manner. This compound shows IC50 values of 1μM in MCF-7 cells and 500nM in NCI-H358 cells.NVP-231 (1μM; 24-72 hours) induces caspase-3 and caspase-9 cleavage in both cell lines. However, the highest caspase-3 and caspase-9 cleavage and activation occurred at 24 hours in MCF-7 cells, then decreases again. In NCI-H358 cells, caspase3 and caspase-9 cleavage occurrs continuously over 72 hours.NVP-231 (0-500nM; 24 hours) causes a concentration-dependent up-regulation of cyclin B1 phosphorylation at Ser133 and a reduction of CDK1 phosphorylation at Tyr15. The total CDK1 expression also declined upon CerK inhibition. Cell Viability Assay Cell Line: MCF-7 cells; NCI-H358 cells Concentration: 0nM, 10nM, 100nM, 300nM, 500nM, 1000nM Incubation Time: 48 hours Result: Reduced MCF-7 cells and NCI-H358 cells in a concentration manner. Apoptosis Analysis Cell Line: MCF-7 cells; NCI-H358 cells Concentration: 1000nM Incubation Time: 24-72 hours Result: Increases caspase-3 and caspase-9 cleavage in MCF-7 and NCI-H358 cells. Western Blot Analysis Cell Line: MCF-7 cells; NCI-H358 cells Concentration: Concentration: 0nM, 100nM, 300nM, 500nM Incubation Time: 24 hours Result: Decreased p-cyclin B1, p-CDK1 as a concentration manner.
保存条件:-20℃