Molecular Weight(MW): 452.51
KD025 is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.
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|Description||KD025 is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.|
KD025 down-regulates the IL-17 and IL-21 secretion in human PBMCs, and leads to down-regulation of STAT3 phosphorylation, IRF4, and RORγt expression in CD4+ T cells.  KD025 inhibits the secretion of IL-21, IL-17, and IFNγ along with decreasing phosphorylated STAT3 and reduced protein expression of IRF4 and BCL6 in human peripheral blood mononuclear cells. 
|In vivo||In mice, KD025 (200 mg/kg, p.o.) inhibits ROCK activity in brain and heart, as measured by the degree of MYPT1 phosphorylation. KD025 (200 mg/kg, p.o.) significantly reduces the area of perfusion defect, and reduces tissue loss in the ipsilateral hemisphere.  In a collagen-induced arthritis (CIA) mouse model, KD025 (200 mg/kg, i.p.) downregulates the progression of collagen-induced arthritis via targeting of the Th17-mediated pathway.  KD025 ()150 mg/kg, i.p. or p.o.) effectively ameliorates cGVHD in a full MHC-mismatch model of multi-organ system cGVHD with bronchiolitis obliterans syndrome and a minor MHC-mismatch model of sclerodermatous GVHD. |
|In vitro||DMSO||90 mg/mL (198.89 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02841995||Recruiting||Graft vs Host Disease||Kadmon Corporation, LLC||August 2016||Phase 2|
|NCT02852967||Recruiting||Psoriasis||Kadmon Corporation, LLC||August 2016||Phase 2|
|NCT02688647||Recruiting||Idiopathic Pulmonary Fibrosis||Kadmon Corporation, LLC||March 2016||Phase 2|
|NCT02557139||Completed||Bioavailability||Kadmon Corporation, LLC|Quotient Clinical||September 2015||Phase 1|
|NCT02317627||Completed||Psoriasis Vulgaris||Kadmon Corporation, LLC||December 2014||Phase 2|
|NCT02106195||Completed||Psoriasis Vulgaris||Kadmon Corporation, LLC||April 2014||Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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