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IWP-2  ≥98%

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包装规格：10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（2 mg/mL 超声）
产品描述：基本信息 产品编号： I10286 产品名称： IWP-2 CAS: 686770-61-6   储存条件 粉末 -20℃ 四年     分子式： C22H18N4O2S3 溶于液体 -80℃ 两年 分子量 466.60 -20℃ 1个月 化学名：  N-(6-Methylbenzo[d]thiazol-2-yl)-2-[(4-oxo-3-phenyl-3,4,6,7-tetrahydrothieno[3,2-d]pyrimidin-2-yl)thio]acetamide Solubility (25°C)：   体外:   DMF 12.5 mg/mL (26.78mM) DMSO Insoluble 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 2.1432mL 10.7158mL 21.4316mL 5mM 0.4286mL 2.1432mL 4.2863mL 10mM 0.2143mL 1.0716mL 2.1432mL   生物活性 产品描述 一种Wnt 加工和分泌的抑制剂，其 IC50 为 27nM。IWP-2 靶向膜结合的 O-酰基转移酶 porcupine (Porcn)，从而阻止关键的 Wnt 配体棕榈糖基化。 靶点 Wnt (Cell-free assay) M82FCK1δ (Cell-free assay) 27nM 40nM 体外研究 IWP-2 inhibits the proliferation of the investigated cell lines within the single digitμM range. IWP-2 inhibits cell proliferation in A818-6, MiaPaCa2, Panc-1, Panc-89, HT29, HEK293, SW620 and Capan cell with EC50s of 8.96μM, 1.90μM, 2.33μM, 3.86 μ M, 4.67μM, 2.76μM, 1.90μM and 2.05μM, respectively. Panc-1 cells are either untreated or treated with 2.33μM IWP-2 for 48 h. In IWP-2 treated cells, the CK1δ kinase peak activity is reduced to approximately 66% residual activity compared to the activity in untreated cells, respectively. IWP-2 reduces the activity of CK1δ in Panc1 cells 体内研究 To evaluate the efficacy of IWP-2 in vivo, 200 μL each of IWP-2-liposome or free liposome i separately injected into C57BL/6 mice intraperitoneally about 2 h before injection of a similar volume of either blue-dye-filled latex beads or E. coli DH5α. IWP-2 causes significant reduction in the uptake of blue beads as well as E. coli as assessed by CFUs in peritoneal lavage cells within 2 h. In addition, the levels of TNF-α and IL-6 in the lavage fluid of the corresponding mice are reduced by 2-4-fold compared with control values. Interestingly, IWP-2 even induces a considerable increase in secretion of the antiinflammatory cytokine IL-10 .   推荐实验方法(仅供参考) Cell Assay The human RCC cell lines 786O and Caki-2 (5×103) are seeded into 96-well plates. Cell viability is estimated by MST assay after Caki-2 acells are incubated with ncreasing concentrations of LEF together with 20μM IWP-2 for 48 h.After treatment, 10 μL MTS is added into each well for 2 h incubation. The absorbance is measured using a model ELX800 Micro Plate Reader at 490nm. For colony formation assay, Caki-2 cells are trypsinized to single cell suspensions and seeded into fresh 6-well plates at 1000 cells/well. Then cells are incubated with LEF at depicted concentrations for 7 days. Colonies are fixed with absolute methanol for 15 min and then stained with 0.1% crystal violet for 20 min. After washing with PBS three times, the colonies with a diameter over 2 mm are visualized by a digital camera
保存条件：-20℃

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