BC-LI-0186 is a potent, specific inhibitor of Leucyl-tRNA synthetase (LRS, LeuRS), inhibits the leucine-dependent mTORC1 pathway.
BC-LI-0186 binds to the RagD interacting site of LRS with KD of 42.1 nM, thereby inhibiting lysosomal localization of LRS and mTORC1 activity.
BC-LI-0186 specifically inhibiting the GTPase activating function of LRS, while not affecting the catalytic activity.
BC-LI-0186binds to the RagD interacting site of LRS, thereby inhibiting lysosomal localization of LRS and mTORC1 activity.
BC-LI-0186 inhibited cancer cell growth human colon cancer SW620 cells with GI50 of 11 nM, inhibited mTORC1 activity, accompanied by PARP or procaspase-3 cleavage.
BC-LI-0186 inhibited the mTORC1 pathway via LRS even in the presence of the known cancer-associated MTOR mutations, overcome acquired rapamycin resistance both in vitro and in vivo.
