NIBR-LTSi is a potent, highly selective and orally active LATS kinase inhibitor with IC50 of 1.4 nM in biochemical CALIPER assay, potently reduces pYAP levels with IC50 of 2.16 uM in JHH5 cells.
NIBR-LTSi robustly reduces YAP phosphorylation and increases proliferation in wild-type (WT) HEK293A cells but not in HEK293A cells with LATS kinase deletion.
NIBR-LTSi (10 uM) promotes primary keratinocyte expansion and blocks differentiation in human 3D skin model.
NIBR-LTSi promotes liver organoid formation (EC50=0.35 uM) and hepatocyte proliferation, NIBR-LTSi-induced YAP signaling enables BEC organoid formation and growth in the absence of WNT/β-catenin-inducing agents.
NIBR-LTSi promotes YAP/TAZ-dependent hepatocyte proliferation and accelerates liver regrowth in AAV8-induced YAP/TAZΔHEP.
NIBR-LTSi induces proliferation of kidney TECs, promotes ISC expansion and blocks their differentiation in organoids and in vivo, accelerates liver regeneration, following partial and extended hepatectomy.