1A-116

**1A-116** is a rationally designed small molecule inhibitor targeting the small GTPase Rac1. It specifically blocks the interaction of Rac1 with its guanine nucleotide exchange factors (GEFs), particularly at the Trp56 binding site, thereby inhibiting Rac1's activation and function. 1A-116 demonstrates antitumor and antimetastatic effects in several cancer types, with a primary focus on malignant gliomas and glioblastoma. It reduces cell proliferation, invasion, and promotes apoptosis in preclinical models. Favorable pharmacokinetic properties include high predicted blood–brain barrier penetration and oral drug-likeness.

Other names

Anti-Rac1 moleculeAnti-Rac-1 moleculeAnti-Rac 1 moleculeRac1 inhibitor 1A-116Rac-1 inhibitor 1A-116Rac 1 inhibitor 1A-116