Tankyrase-IN-2 |
| Catalog No.GC37735 |
A TNKS1/2 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1588870-36-3
Sample solution is provided at 25 µL, 10mM.
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Tankyrase-IN-2 (compound 5k) is a potent, selective, and orally active tankyrase inhibitor (IC50s of 10, 7, and 710 nM for TNKS1, TNKS2 as well as PARP1, respectively). Tankyrase-IN-2 has favorable physicochemical profile and pharmacokinetic properties modulating Wnt pathway activity in a colorectal xenograft model[1]. IC50: 10 nM (TNKS1), 7 nM (TNKS2), 710 nM (PARP1)[1]
Tankyrase-IN-2 (1-10000 nM; 24 hours) leads to a dose-dependent increase of tankyrase protein abundance with an EC50 of 320 nM in DLD1 cells. This is in the same potency range as the value for axin2 increase (EC50=319 nM)[1].
[1]. Buchstaller HP, et al. Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective TankyraseInhibitor Modulating Wnt Pathway Activity. J Med Chem. 2019 Aug 5.
Average Rating: 5 (Based on Reviews and 10 reference(s) in Google Scholar.)
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