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JW 55 (JW55) 是一种有效且选择性的 β-catenin 信号通路抑制剂,通过抑制 tankyrase 1 和 tankyrase 2 (TNKS1/2) 的 PARP 结构域起作用。
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JW 55 (JW55) 是一种有效且选择性的 β-catenin 信号通路抑制剂,通过抑制 tankyrase 1 和 tankyrase 2 (TNKS1/2) 的 PARP 结构域起作用。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 119 | 现货 | |
10 mg | ¥ 208 | 现货 | |
25 mg | ¥ 413 | 现货 | |
50 mg | ¥ 672 | 现货 | |
100 mg | ¥ 1,090 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 137 | 现货 |
产品描述 | JW 55 (JW55) is an effective and selective β-catenin signaling pathway inhibitor, works by inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). |
靶点活性 | TNKS2 (auto-PARsylation):830 nM, TNKS1 (auto-PARsylation):1.9 μM |
体外活性 | JW55是一种针对经典Wnt通路的强效且选择性的抑制剂。在Wnt3a诱导并瞬时转染有ST-Luc(SuperTop-萤火虫素酶)报告基因的HEK293细胞中,JW55展现出以IC50值为470 nM的抑制作用。在SW480细胞中,JW55在1至5μM范围内有效;而在HCT-15细胞中,有效范围扩展至0.01至5μM[1]。 |
体内活性 | JW 55(100 mg/kg,口服)减缓了条件性Apc基因敲除小鼠的肿瘤发展。JW 55减少了Xenopus胚胎中XWnt8诱导的轴向复制和Tamoxifen诱导的条件性APC突变小鼠中的息肉形成[1]。 |
细胞实验 | JW 55 (JW55) is prepared in DMSO and stored, and then diluted with appropriate medium[1]. A total of 1,000 SW480 or RKO cells are seeded in 96-well plates. The day after, the cell culture medium is exchanged to solutions that contained 0.1% DMSO or 10 μM JW55 for RKO cells and 0.1% DMSO or 10, 5, or 1 μM JW55 for SW480 cells. All samples consist of a minimum of 6 replicates. The plate is incubated in an IncuCyte inside a cell culture incubator. Images are captured every second hour to monitor proliferation[1]. |
别名 | JW55 |
分子量 | 434.48 |
分子式 | C25H26N2O5 |
CAS No. | 664993-53-7 |
Smiles | COc1ccc(cc1)C1(CNC(=O)c2ccc(NC(=O)c3ccco3)cc2)CCOCC1 |
密度 | 1.235 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 100 mM DMSO: 50 mg/mL (115.08 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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