RKI-1447

RKI-1447 is a potent, selective, small molecule inhibitor of Rho-associated coiled-coil containing protein kinases 1 and 2 (ROCK1 and ROCK2), with IC50 values of 14.5 nM and 6.2 nM, respectively. Developed by researchers at the H. Lee Moffitt Cancer Center and Research Institute and the University of South Florida, RKI-1447 functions as a Type I kinase inhibitor that binds to the ATP-binding site of the kinase, interacting with the hinge region and the DFG motif. It suppresses the phosphorylation of downstream ROCK substrates, such as myosin light chain 2 (MLC2) and myosin phosphatase target subunit 1 (MYPT1), without affecting other signaling pathways like AKT, MEK, or S6 kinase. Preclinical studies have demonstrated that RKI-1447 exhibits significant anti-invasive and anti-tumor activities in breast cancer, colorectal carcinoma, medulloblastoma, and other malignancies. Additionally, it has been investigated for its potential to lower intraocular pressure in glaucoma models, alleviate spinal cord injury-related impairments, and modulate insulin resistance and inflammation in nonalcoholic fatty liver disease (NAFLD).

Other names

1-[(3-hydroxyphenyl)methyl]-3-(4-pyridin-4-yl-1,3-thiazol-2-yl)ureaRKI 1447RKI1447RKI-1447RKI-1447 dihydrochlorideRKI1447 dihydrochlorideRKI 1447 dihydrochloride