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基本信息
安全信息
存储条件Freezer -20℃ | Symbol  |
Signal WordWarning | Hazard StatementsH315 H319 H335 |
Precautionary StatementsP280 P321 P261 P271 P319 P405 P501 P302+P352 P332+P317 P362+P364 P264+P265 P305+P351+P338 P337+P317 P304+P340 P403+P233 | |
化学和物理性质
产品描述
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.
