Drug intelligence / Profile preview

RKI-18

Development stage
Preclinical
Lead developer
Moffitt Cancer Center
Modality
Small Molecules
Administration
Parenteral
01

Overview

RKI-18 is a potent, small molecule inhibitor of Rho-associated protein kinases 1 and 2 (ROCK1 and ROCK2), with IC50 values of 397 nM and 349 nM, respectively. Developed by researchers at the Moffitt Cancer Center and the University of South Florida, RKI-18 acts as an ATP-competitive inhibitor that suppresses the phosphorylation of myosin light chain 2 (MLC2), a key downstream substrate of ROCK. By inhibiting ROCK-mediated signaling, RKI-18 prevents actin stress fiber formation, lamellipodia, and filopodia formation, thereby suppressing the migration, invasion, and anchorage-independent growth of human cancer cells, particularly breast, lung, colon, and prostate cancer cells.

Other names
RKI 18RKI18RKI-18Rho-kinase inhibitor 18
02

Targets

ROCK1 (Rho-associated coiled-coil containing protein kinase 1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)

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