INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT.

2016年4月5日 · A rescue experiment confirmed that INI-43 exerted its cell killing effects, in part, by targeting Kpnβ1. INI-43 treatment elicited a G 2 –M cell-cycle arrest in cancer cells and induced the intrinsic apoptotic pathway. Intraperitoneal administration of INI-43 significantly inhibited the growth of subcutaneously xenografted esophageal and ...

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 G 2 -M cell cycle arrest in cancer cells, and induce …

INI-43 treatment elicited a G2-M cell-cycle arrest in cancer cells and induced the intrinsic apoptotic pathway. Intraperitoneal administration of INI-43 significantly inhibited the growth of subcutaneously xenografted esophageal and cervical tumor cells. We propose that Kpnβ1 inhibitors could have therapeutic potential for the treatment of cancer.

2021年2月2日 · Inhibition of nuclear import via Karyopherin beta 1 (Kpnβ1) shows potential as an anti-cancer approach. This study investigated the use of nuclear import inhibitor, INI-43, in combination with cisplatin. Cervical cancer cells were pre-treated with INI-43 before treatment with cisplatin, and MTT cell viability and apoptosis assays performed.

INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT.

INI-43 是Nuclear Import-43 的抑制剂，通过靶向 Kpnβ1 对各种宫颈和食管癌细胞系显示出显着的细胞毒性作用，并干扰 Kpnβ1 和已知的 Kpnβ1 cargo 蛋白、NFAT、NFκB、AP-1和NFY 的核定位。

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.

INI-43 is a cell penetrant and potent inhibitor of Kpnb1-mediated nuclear import that cancer cell death via a G2–M cell cycle arrest followed by apoptosis. INI-43 inhibits the nuclear localization of Kpnb1 as well as that of its cargo transcription factors, NFY, AP-1, p65, and NFAT.