NCIt definition : An orally bioavailable inhibitor of Rho-associated coiled-coil kinase 2 (ROCK2; ROCK-II),
with potential immunomodulating activity. Upon oral administration, belumosudil binds
to and inhibits the serine/threonine kinase activity of ROCK2. This inhibits ROCK2-mediated
signal transduction pathways and modulates various pro- and anti-inflammatory immune
cell responses through the regulation of signal transducer and activator of transcription
3 and 5 (STAT3/STAT5) phosphorylation. This downregulates pro-inflammatory Th17 cells
and increases regulatory T (Treg) cells. Belumosudil also inhibits ROCK2-mediated
fibrotic processes, including stress fiber formation, myofibroblast activation and
pro-fibrotic gene transcription. ROCK2 is upregulated in various diseases, including
various fibrotic, neurodegenerative and autoimmune diseases.;
UNII : 834YJF89WO;
InChIKey : GKHIVNAUVKXIIY-UHFFFAOYSA-N;
CAS number : 911417-87-3;
Molecule name : SLx 2119; KD 025; SLx-2119; KD-025;