Drug intelligence / Profile preview

UI-152

Development stage
Preclinical
Lead developer
Incheon National University
Modality
Small Molecules
01

Overview

UI-152 is a small molecule inhibitor of the oncogenic BRAF kinase, specifically targeting the BRAF-V600E mutation. Developed through a collaboration between researchers at the University of Incheon and Virginia Tech, UI-152 has demonstrated high potency in biochemical assays, inhibiting BRAF-V600E at low nanomolar concentrations and showing approximately 10-fold greater potency than the established BRAF inhibitor vemurafenib (PLX4032). In preclinical studies using malignant glioma cell lines, UI-152 selectively inhibited the proliferation of cells harboring the BRAF-V600E mutation while causing paradoxical activation of the MAPK pathway in wild-type BRAF cells. This profile suggests UI-152 as a potential therapeutic candidate for brain tumor patients with specific genetic profiles.

02

Targets

BRAF (B-Raf proto-oncogene, serine/threonine kinase)ARAF (Proto-oncogene serine/threonine-protein kinase A-Raf)

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