Belumosudil mesylate

Names

[ Name ]:
Belumosudil mesylate

Biological Activity

[Description]:

Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties[1].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

ROCK2:105 nM (IC50)

ROCK1:24 μM (IC50)

[In Vitro]

Belumosudil (SLx-2119; 40 µM) induces significant down-regulations of Tsp-1 and CTGF mRNA levels in PASMC. The microarray hybridized with aRNA from HMVEC treated with Belumosudil, shows a 5-times higher background than the other arrays[1].

[In Vivo]

Belumosudil (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. Belumosudil is at least as efficacious in aged, diabetic or female mice, as in normal adult males[2].

[References]

[1]. Boerma, M., et al. Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase. Blood Coagul Fibrinolysis. 2008 Oct;19(7):709-18.

[2]. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₇H₂₈N₆O₅S

[ Molecular Weight ]:
548.61

Related Compounds

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