Belumosudil
ROCK2 inhibitor / Selective inhibitor of Rho kinase 2 (ROCK2) – IC50’s: ROCK2 = 105 nM, ROCK1 = 24 µM in enzyme assays.1 It downregulated the ability of T cells to secrete IL-21 and IL-17, but not IFN-g, in response to T cell stimulation in vitro via a STAT3-dependent mechanism.2 Belumosudil ameliorated graft-versus-host disease in multiple models3,4 and was recently approved by the FDA for the treatment of GVHD (July 2021). It has also been shown to suppress adipogenesis.5-7 Suppression of adipocyte differentiation is mediated via casein kinase 2 inhibition (IC50 = 50 nM) and not ROCK2 inhibition.8
Biochemicals & reagents
911417-87-3
KD025; SLx-2119
Boerma et al. (2008) Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin; Blood Coagul. Fibrinolysis. 19 709 Zanin-Zhorov et al. (2014) Selective oral ROCK2 inhibitor down-regulates IL-21 and IL-17 secretion in human T cells via STAT3-dependent mechanism; Natl. Acad. Sci. USA 111 16814 Flynn et al. (2016) Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism; 127 2144 Jagasia et al. (2021) ROCK2 Inhibition with Belumosudil (KD025) for the Treatment of Chronic Graft-Versus-Host Disease; Clin. Invest. 39 1888 Diep et al. (2018) Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells; Rep. 8 2477 Diep et al. (2019) KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells; Adipocyte 9 114 Wei et al. (2020) ROCK2 inhibition enhances the thermogenic program in white and brown fat tissue in mice; FASEB J. 34 474 Tran and Chun (2021) ROCK2-Specific Inhibitor KD025 Suppresses Adipocyte Differentiation by Inhibiting Casein Kinase 2; Molecules 26 4747
-20°C
TARGET: Kinase -- PATHWAY: Wnt -- RESEARCH AREA: Immunology; Angiogenesis -- DISEASE AREA: Inflammation; Ischemia