Belumosudil (KD025)

For research use only.

Catalog No.S7936 Synonyms: SLx-2119

4 publications

Belumosudil (KD025) Chemical Structure

CAS No. 911417-87-3

Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.

Selleck's Belumosudil (KD025) has been cited by 4 publications

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Biological Activity

Description Belumosudil (KD025, SLx-2119) is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nM, respectively. Phase 2.
ROCK2 [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
41 nM(Ki) 60 nM
In vitro

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. [2] 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. [3]

Methods Test Index PMID
Western blot
pSTAT3 / Bcl6 / pSTAT5 / Blimp1 ; 

PubMed: 27436361     

PBMCs from six active SLE patients were treated with the indicated concentrations of KD025 for 1 hour and then were stimulated under Th17-type skewing conditions. (B to E) The cells were analyzed by Western blotting with antibodies specific for (B) pSTAT3 (n = 5), (C) Bcl6 (n = 4), (D) pSTAT5 (n = 3), and (E) Blimp1 (n = 3). Statistical analysis was performed with the Wilcoxon test.

IL-21 / IL-17 / IFN-γ; 

PubMed: 25385601     

Peripheral blood CD4+ T cells were treated with selective ROCK2 inhibitor KD025 for 1 h and then stimulated by anti-CD3/28 mAbs alone. IL-21, IL-17, and IFN-γ secretion was analyzed by ELISA after 48 h.

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. [1] 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. [2] 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. [3]


Animal Research:


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  • Animal Models: Young adult, aged, or type 2 diabetic mice
  • Dosages: 300 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (198.89 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+35% PEG 300+2%Tween 80+ddH2O
For best results, use promptly after mixing.

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 452.51


CAS No. 911417-87-3
Storage powder
in solvent
Synonyms SLx-2119
Smiles CC(C)NC(=O)COC1=CC=CC(=C1)C2=NC3=CC=CC=C3C(=N2)NC4=CC5=C(C=C4)NN=C5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02557139 Completed Drug: KD025 Tablet|Drug: KD025 as drug in capsule Bioavailability Kadmon Corporation LLC|Quotient Clinical September 2015 Phase 1
NCT02317627 Completed Drug: KD025 Psoriasis Vulgaris Kadmon Corporation LLC December 2014 Phase 2

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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.

Handling Instructions

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ROCK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID