| Description | G244-LM is a potent and specific inhibitor of tankyrase 1/2. G244-LM inhibits Wnt signaling. |
| In vitro | G244-LM is a potent and specific small-molecule tankyrase inhibitors, that reduce Wnt/β-catenin signaling by preventing poly(ADP-ribosyl)ation-dependent AXIN degradation, thereby promoting β-catenin destabilization.?The novel tankyrase inhibitors completely block ligand-driven Wnt/β-catenin signaling in cell culture and display approximately 50% inhibition of APC mutation-driven signaling in most CRC cell lines.?It was previously unknown whether the level of AXIN protein stabilization by tankyrase inhibition is sufficient to impact tumor growth in the absence of normal APC activity. |
| molecular weight | 406.52 |
| Molecular formula | C18H22N4O3S2 |
| CAS | 1563007-08-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5 mM |
| References | 1. Lau T , Chan E , Callow M , et al. A Novel Tankyrase Small-Molecule Inhibitor Suppresses APC Mutation–Driven Colorectal Tumor Growth[J]. Cancer Research, 2013, 73(10):3132-3144. |