UNC10245380 (UNC5380) is a small molecule ligand/inhibitor of Calcium and Integrin Binding protein 1 (CIB1) with IC50 of 8.0 uM in TR-FRET displacement assay, selectively kills CIB1 depletion-sensitive TNBC cells.
UNC10245380 shows significant cell killing activity in both CIB1-depletion-sensitive (MDA-MB-461, and MDA-MB-468) cell lines.
UNC10245380 shows no activity in the CIB1-depletion-insensitive (MDA-MB-231) cell line.
UNC10245380 also shows >90% dose-dependent cell death of MDA-468 TNBC cells over 48 h, indicating a more robust and rapid cell death than CIB1 shRNA depletion by 72 h.
UNC10245380 inhibits AKT and ERK phosphorylation in CIB1 depletion-sensitive, but not insensitive cell lines.
) upregulates γH2AX and inhibits AKT and ERK phosphorylation in CIB1 depletion-sensitive, but not insensitive cell lines.
UNC10245380 closely parallels the CIB1 depletion cell death and signaling phenotypes in TNBC cells.