Drug intelligence / Profile preview

ini-43

Development stage
Preclinical
Lead developer
University of Cape Town
Modality
Small Molecules
Administration
In Vitro (cell Culture Studies)
01

Overview

**INI-43** is a small molecule inhibitor of nuclear import that targets **Karyopherin beta 1 (Kpnβ1)**, a nuclear import protein responsible for transporting cargo from the cytoplasm into the nucleus[1][2][3]. Kpnβ1 is overexpressed in multiple cancer types, and its inhibition by INI-43 disrupts nuclear import, cell survival, and proliferation. INI-43 has shown anti-cancer effects in both cell culture and animal models, causing apoptosis and sensitizing cancer cells—such as cervical cancer cells—to cisplatin therapy via stabilization of **p53** and inhibition of **NFκB** nuclear translocation, resulting in enhanced DNA damage and cell death[1][2][3]. INI-43 binds directly to Kpnβ1 and also appears to interact with the nuclear import protein IPO5, without binding to other import proteins tested[2].

Other names
Inhibitor of Nuclear Import INI-43
02

Targets

IPO5 (Importin-5)RELA (Nuclear Factor Kappa B Subunit p65)KPNB1 (Importin subunit beta-1)TP53 (Cellular Tumor Antigen p53 R175H)

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