生物活性
JW 55 is a potent and selective β-catenin signaling pathway inhibitor, which functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2). JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively.
IC50 & Target[1]
TNKS2
0.83 μM (IC50)
TNKS1
1.9 μM (IC50)
体外研究(In Vitro)
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
体内研究
(In Vivo)
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].
分子量
434.48
性状
Solid
Formula
C25H26N2O5
CAS 号
664993-53-7
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 50 mg/mL (115.08 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 2.3016 mL 11.5080 mL 23.0160 mL
5 mM 0.4603 mL 2.3016 mL 4.6032 mL
10 mM 0.2302 mL 1.1508 mL 2.3016 mL
*
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。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: