Drug intelligence / Profile preview

1-(1H-indazol-5-yl)-3-phenylurea

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

Overview

RKI-11 is a small molecule indazole urea-based compound that acts as a weak or inactive analogue of the Rho-associated kinase (ROCK) inhibitor RKI-18. Developed by researchers at the Moffitt Cancer Center, RKI-11 inhibits ROCK1 and ROCK2 with low potency, exhibiting IC50 values of 38 µM and 45 µM, respectively. Due to its minimal activity in suppressing the phosphorylation of the ROCK substrate myosin light chain 2 (MLC2) and its lack of effect on cancer cell migration and invasion, RKI-11 is widely utilized as a negative control or chemical probe in preclinical studies investigating the therapeutic potential of ROCK inhibition in oncology.

Other names
1-(1H-indazole-5-yl)-3-phenylurea1-(1H-indazol-5-yl)-3-phenylurea3-(1H-indazol-5-yl)-1-phenylurea
02

Targets

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

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