Belumosudil is a selective inhibitor of Rho kinase 2 (ROCK2) - IC50s: 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
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