JW 55

"

Cell Cycle/DNA DamageEpigenetics-

JW 55 ?????????????????????????????-catenin??????????????????????????????????????? (tankyrase 1 ??? tankyrase 2???TNKS1/2) ???????????????

PARP

相关产品

Olaparib-BMN-673-MK-4827-XAV-939-Rucaparib phosphate-Nicotinamide-PJ34 hydrochloride-Veliparib dihydrochloride-NVP-TNKS656-AZD-2461-E7449-BSI-201-G007-LK-INO-1001-A-966492-

生物活性

Description

JW 55 is a potent and selective??-cateninsignaling 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 withIC50s of 1.9 ??M and 830 nM respectively.

IC50& Target

IC50: 1.9 ??M (TNKS1); 830 nM (TNKS2)[1]

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 IC50value of 470 nM. JW55 is effective in the range of 1 to 5 ??M in SW480 cells and 0.01 to 5 ??M in HCT-15 cells. JW55 is effective in the range of 1 to 5 ??M in SW480 cells and 0.01 to 5 ??M in HCT-15 cells[1].

In Vivo

JW 55 (100 mg/kg, orally) reduces tumor development in conditionalApcknockout mice. JW55 reduces XWnt8-induced axis duplication inXenopusembryos and Tamoxifen-induced polyposis formation in conditional APC mutant mice[1].

References

[1].Waaler J, et al. A novel tankyrase inhibitor decreases canonical Wnt signaling in colon carcinoma cells and reduces tumor growth in conditional APC mutant mice. Cancer Res. 2012 Jun 1;72(11):2822-32.