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Cell Cycle/DNA DamageEpigenetics-
JW 55 ?????????????????????????????-catenin??????????????????????????????????????? (tankyrase 1 ??? tankyrase 2???TNKS1/2) ???????????????
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
