FiVe1

FiVe1 is a vimentin (VIM) inhibitor. FiVe1 binds to the rod domain of VIM, causing metaphase VIM disassembly and hyperphosphorylation at Ser56, ultimately leading to mitotic catastrophe, multinucleation, and loss of stemness. FiVe1 has anticancer activity against soft tissue sarcomas. FiVe1 increases the sensitivity of ovarian cancer to Cisplatin (HY-17394). FiVe1 can be used for researches of mesenchymal cancers (including breast cancer and soft tissue sarcoma) and ovarian cancers^[1][2][3]. IC50 & Target:IC50: VIM^[1] In Vitro:FiVe1 (2 μM; 72 h) selectively inhibits the growth of FOXC2-HMLER cells while showing little toxicity to HMLER cells^[1].
FiVe1 (250 nM) results in a collapsed VIM filamentous structure in FOXC2-HMLER cells^[1].
FiVe1 (1 μM for multinucleation test; 24 h for multinucleation test) inhibits the growth of multiple soft tissue sarcoma (STS) cell lines (HT1080, SW684, RD, GCT, SW872, SW982) and promotes multinucleation in these cell lines, respectively^[1].
FiVe1 (72 h) inhibits the growth of HUVECs and human lung fibroblasts (HLFs), with IC₅₀ values of 1.70 μM and 2.32 μM, respectively^[1].
FiVe1 inhibits the growth of HT-1080 fibrosarcoma cells, with an IC₅₀ of 1.6 μM^[2].
FiVe1 (0.2 μM; 72 h) significantly sensitizes both A2780 and A2780cis cells towards Cisplatin (HY-17394)^[3].