INI-43

INI-43 is an inhibitor of Kpnβ1, interfering with the nuclear localization of Kpnβ1 and known Kpnβ1 cargo proteins, NFAT, NFκB, AP-1, and NFY. INI-43 can inhibit the proliferation of cancer cells, cause G₂-M cell cycle arrest in cancer cells, and induce the intrinsic apoptosis pathway^[1][2][3]. In Vitro:INI-43 (5 μM, 2h) pretreatment n HeLa and SiHa cell lines of cervical cancer can effectively reduce the nuclear accumulation and activity of NFκB, resulting in decreased expression of cyclin D1, c-Myc and XIAP, and impaired DNA repair ability. Make cells more sensitive to Cisplatin^[2].
INI-43 (10, 15 μmol/L, 1.5, 3h) interferes with the entry of Kpnβ1, NFAT, p65 and NFY into the nucleus and induces apoptosis in HeLa cells. The IC₅₀ value of INI-43 against HeLa cells is 9.3 μmol/L^[3].
INI-43 (5, 10 μmol/L, 5 days) has different sensitivity to cancer cell lines (cervical and esophageal cancer) and non-cancer lines (DMB and FG0), and INI-43 can kill cancer cells and has no effect on non-cancer cells^[3].
In Vivo:INI-43 has good metabolic stability with a degradation half-life of more than 100 minutes and a maximum tolerable dose (MTD) of 50 mg/kg^[3].
INI-43 (50 mg/kg, intrabitoneal injection, once every 2-3 days, for 3 to 4 weeks) can inhibit tumor growth in mouse tumor xenotransplantation model ^[3].