EHop-016是Rac GTP酶Rac1和Rac3的有效选择性抑制剂。它在MDA-MB-435细胞中抑制Rac1活性的IC50为1.1 μM。EHop-016抑制Vav2与Rac的相互作用、Rac介导的PAK1活化、片状脂蛋白形成和细胞迁移。

EHT 1864 2HCl is an inhibitor of Rac1 (Kd = 40 nM), Rac1b (Kd = 50 nM), Rac2 (Kd = 60 nM) and Rac3 (Kd = 250 nM).

Azathioprine can inhibit GTP-binding protein Rac1 activation and purine synthesis. Azathioprine is used to treat organ transplantation and autoimmune diseases.

NSC23766 is identified to fit into a surface groove of Rac1 known to be critical for GEF specification.