Drug intelligence / Profile preview

RKI-1313

Development stage
Unknown
Lead developer
Moffitt Cancer Center
Modality
Small Molecules
Administration
Topical
01

Overview

RKI-1313 is a small-molecule inhibitor of Rho-associated coiled-coil–containing protein kinases (ROCK1 and ROCK2), with moderate selectivity for ROCK2 (IC50 values of 34 µM and 8 µM, respectively). Developed by the H. Lee Moffitt Cancer Center & Research Institute, RKI-1313 is a structurally-related analog of the more potent ROCK inhibitor RKI-1447. Due to its relatively weak potency and minimal effect on downstream phenotypes such as substrate phosphorylation, cell migration, invasion, and anchorage-independent growth, RKI-1313 is primarily utilized as a negative control or chemical probe in research settings to delineate ROCK-dependent signaling pathways in cancer models.

Other names
N-[(3-methoxyphenyl)methyl]-N'-[4-(4-pyridinyl)-2-thiazolyl]-urea
02

Targets

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

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