KD025 (Belumosudil, SLx-2119) is a potent, selective ROCK2 inhibitor with IC50 of 105 nM.
KD025 displays >200-fold selectivity over ROCK1 (IC50>20 uM).
KD025 dose-dependently reduced infarct volume after transient middle cerebral artery occlusion, cortical perfusion in a distal middle cerebral artery occlusion model.
KD025 significantly diminished STAT3 phosphorylation and binding to IL-17 and IL-21 promoters and reduced IRF4 and nuclear hormone RAR-γt protein levels in T cells derived from healthy subjects or rheumatoid arthritis patients.
KD025 in vivo down-regulates the progression of collagen-induced arthritis in mice via targeting of the Th17-mediated pathway.
KD025 inhibits the secretion of IL-21, IL-17, and INF-γ along with decreasing p-STAT3 and reduced protein expression of IRF4 and BCL6 in human PBMCs purified from active cGVHD patients.
