JW 55 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。
产品描述
JW 55 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).
体外活性
JW 55 (JW55) is a potent and selective inhibitor of the canonical Wnt pathway. Wnt3a-induced HEK293 cells containing a transiently transfected ST-Luc (SuperTop-luciferase) reporter show inhibition by JW55 with an IC50 value of 470 nM. JW55 is effective in the range of 1 to 5 μM in SW480 cells and 0.01 to 5 μM in HCT-15 cells. JW55 is effective in the range of 1 to 5 μM in SW480 cells and 0.01 to 5 μM in HCT-15 cells[1].
体内活性
JW 55 (100 mg/kg, orally) reduces tumor development in conditional Apc knockout mice. JW55 reduces XWnt8-induced axis duplication inXenopus embryos and Tamoxifen-induced polyposis formation in conditional APC mutant mice[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].
Cas No.
664993-53-7
分子式
C25H26N2O5
分子量
434.48
别名
JW55
储存和溶解度
DMSO:100 mM
Ethanol:100 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years