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JW 55
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
JW 55图片
CAS NO:664993-53-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 434.48
Formula C25H26N2O5
CAS No. 664993-53-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 10 mM
Water: <1 mg/mL
Ethanol:
SMILES Code O=C(C1=CC=CO1)NC2=CC=C(C(NCC3(C4=CC=C(OC)C=C4)CCOCC3)=O)C=C2
Synonyms JW55; JW-55; JW 55
实验参考方法
In Vitro

In vitro activity: JW 55 is a potent and selective small molecule inhibitor of β-catenin signaling pathway, it functions via inhibition of the PARP domain of tankyrase 1 and tankyrase 2 (TNKS1/2) which are regulators of the β-catenin destruction complex. JW 55 decreases auto-PARsylation of TNKS1/2 in vitro with IC50s of 1.9 μM and 830 nM respectively. Inhibition of TNKS1/2 poly(ADP-ribosyl)ation activity by JW55 led to stabilization of AXIN2, a member of the β-catenin destruction complex, followed by increased degradation of β-catenin. JW55 inhibited canonical Wnt signaling in a dose-dependent manner in colon carcinoma cells that contained mutations in either the APC (adenomatous polyposis coli) locus or in an allele of β-catenin. In addition, JW55 reduced XWnt8-induced axis duplication in Xenopus embryos and tamoxifen-induced polyposis formation in conditional APC mutant mice.


Kinase Assay: 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


Cell Assay: 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.

In VivoJW 55 at 100 mg/kg 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
Animal model Female Apc knockout mice (ApcCKO/CKO/Lgr5-CreERT2 mice)
Formulation & Dosage 100 mg/kg; oral
References Cancer Res. 2012 Jun 1;72(11):2822-32.