Belumosudil mesylate (KD025 mesylate) is a compound that selectively inhibits ROCK2, demonstrating IC50 values of 105 nM for ROCK2 and 24 μM for ROCK1. It possesses anti-fibrotic properties.

ROCK1:24 μM (IC50), ROCK2:105 nM (IC50)

Belumosudil (SLx-2119; 40 μM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays[1].

Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males[2].