产品描述

JW55是一种有效的、选择性经典Wnt信号通路抑制剂，通过抑制TNKS1/2的PARP区域发挥作用。

靶点（IC50 & Targe）

TNKS1,1.9μM

TNKS2,830nM

体外研究

JW55 inhibits the PARP domain of TNKS1/2, leading to the stabilization of AXIN2 followed by increased degradation of β-catenin. Wnt3a-induced HEK293 cells containing a transiently transfected ST-Luc (SuperTop-luciferase) reporter show inhibition by JW55 with an IC50 value of 470 nmol/L. JW55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50 values of 1.9 μmol/L and 830 nmol/L, respectively. JW55-mediated inhibition of canonical Wnt signaling results in reduced cell-cycle progression, proliferation, and colony formation in the CRC cell line SW480 in vitro[1].

体内研究

JW55 reduces XWnt8-induced axis duplication in Xenopus embryos and tamoxifen-induced polyposis formation in conditional APC mutant mice[1].

细胞实验

Cell lines: SW480 cells

Concentrations: 10, 5, or 1 μmol/L

Incubation Time: 9 days

Method:--

(Only for Reference)

动物实验

Animal Models: Apc(CKO/CKO)Lgr5-CreERT2+ mice

Formulation: DMSO

Dosages: 100 mg/kg

Administration: oral

(Only for Reference)

参考文献

[1] Waaler J, et al. Cancer Res. 2012, 72(11):2822-32.