TC13172 is a mixed lineage kinase domain-like protein (MLKL) inhibitor with an EC50 value of 2 nM for HT-29 cells.
The anti-necroptosis potency of TC13172 is evaluated in the HT-29 cell line, the EC50 value is 2±0.6 nM. TC13172 has an inhibition potency of 2 nM against cell necroptosis. TC13172 inhibits MLKL by directly binding to Cys-86. TC13172 does not disrupt the phosphorylation of MLKL, but do decrease the level of MLKL in the membrane phase, demonstrating that these MLKL inhibitors block the translocation of MLKL to the cell membrane, thereby protecting cells from necroptosis[1].
[1]. Bo Yan, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein.ChemCommun (Camb). 2017 Mar 28;53(26):3637-3640.