KD 025

KD 025 is an inhibitor of Rho-associated kinase 2 (ROCK2; IC₅₀ = 0.105 µM).¹ It is selective for ROCK2 over ROCK1 (IC₅₀ = 24 µM). KD 025 (10 µM) decreases the expression of connective tissue growth factor (CTGF) and induces remodeling of the actin cytoskeleton in isolated human ileal fibrotic smooth muscle cells. It inhibits heat-killed C. albicans- or S. epidermidis-induced production of IL-17 in isolated human peripheral blood mononuclear cells (PBMCs) when used at concentrations ranging from 1.25 to 10 µM.² KD 025 (100 and 200 mg/kg) reduces infarct volume in a mouse model of cerebral ischemia induced by transient middle cerebral artery occlusion (MCAO).³ It decreases disease severity in a mouse model of sclerodermatous chronic graft versus host disease (GVHD) when administered at a dose of 150 mg/kg.⁴ Formulations containing KD 025 have been used in the treatment of chronic GVHD.

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1. Boerma, M., Fu, Q., Wang, J., et al. 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(7), 709-718 (2008).

2. Tengesdal, I.W., Kitzenberg, D., Li, S., et al. The selective ROCK2 inhibitor KD025 reduces IL-17 secretion in human peripheral blood mononuclear cells independent of IL-1 and IL-6. Eur. J. Immunol. 48(10), 1679-1686 (2018).

3. Wang, H., Zhang, D., Ge, M., et al. Formononetin inhibits enterovirus 71 replication by regulating COX-2/PGE₂ expression. Virol. J. 12, 35 (2015).

4. Flynn, R., Paz, K., Du, J., et al. Targeted Rho-associated kinase 2 inhibition suppresses murine and human chronic GVHD through a Stat3-dependent mechanism. Blood 127(17), 2144-2154 (2016).