Catalog No.: PC-22213Not For Human Use, Lab Use Only.
NCT-58 is a specfiic small molecule C-terminal HSP90 inhibitor, kills trastuzumab-resistant HER2-positive breast cancer stem-like cells, targets the C-terminal HSP90 without inducing heat shock response (HSR).
NCT-58 is a specfiic small molecule C-terminal HSP90 inhibitor, kills trastuzumab-resistant HER2-positive breast cancer stem-like cells, targets the C-terminal HSP90 without inducing heat shock response (HSR). NCT-58 exhibits significant inhibition of cell proliferation in HER2-positive breast cancer cells, with an IC50 = 8.53 and 4.45 μM in BT474 and JIMT1, respectively, with minimal cytotoxicity in normal HEK293 cells. NCT-58 targets the C-terminal domain of HSP90 and downregulates HER2, HER3, and EGFR expression. NCT-58 induces apoptosis and inhibits tyrosine kinase activity of HER2 in trastuzumab-resistant cells. NCT-58 eradicates HER2-positive BCSCs without triggering the HSR. NCT-58 (30 mg/kg) inhibits tumor growth in trastuzumab-resistant JIMT-1 xenografts, suppresses BCSC-like properties and downregulates the expression of HSF-1, HSP70, and HSP90 in vivo.
