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GSK429286A
- Development stage
- Unknown
- Lead developer
- GSK
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
GSK429286A is a potent, selective, and orally active small molecule inhibitor of Rho-associated coiled-coil containing protein kinase 1 (ROCK1) and ROCK2, with IC50 values of 14 nM and 63 nM, respectively. Developed by GSK, the compound is widely utilized as a chemical biology research tool to investigate the Rho/ROCK signaling pathway, which plays a critical role in regulating cytoskeletal dynamics, cell migration, and smooth muscle contraction. In preclinical studies, GSK429286A has demonstrated significant vasodilatory and antihypertensive effects, reducing mean arterial pressure in spontaneously hypertensive rats, and has shown therapeutic potential in promoting collateral vessel growth and functional recovery in models of lower limb ischemia.
- Other names
- GSK 429286GSK429286GSK-429286GSK 429286AGSK429286AGSK-429286ARHO-15RHO15RHO 15
02
Targets
ROCK1 (Rho-associated coiled-coil containing protein kinase 1)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)RPS6KA1 (Ribosomal S6 kinase Alpha-1)RPS6KB1 (Ribosomal protein S6 kinase beta-1)
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