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Belumosudil

Catalog No. T6867 CAS 911417-87-3

Synonyms: KD025, Rezurock, ROCK inhibitor, SLx-2119

Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Belumosudil, CAS 911417-87-3

Pack Size	Availability	Price/USD
2 mg	In stock	$ 41.00
5 mg	In stock	$ 67.00
10 mg	In stock	$ 92.00
25 mg	In stock	$ 169.00
50 mg	In stock	$ 263.00
100 mg	In stock	$ 396.00
500 mg	In stock	$ 943.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 98.59%

Purity: 98.37%

Purity: 97.41%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).
Targets&IC50	ROCK2:41 nM(Ki), ROCK2:60 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]
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]
Kinase Assay	Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 μM ATP, containing?33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450.
Cell Research	SLx-2119 is dissolved in DMSO to obtain a stock solution of 20 mM. Western blots are used to determine whether HMVEC, NHDF and PASMC express ROCK1 and ROCK2. The cells are incubated for 24 hours in 3 mL culture media containing SLx-2119. All cells are collected at passage 3 and lysed on ice in 25 mM Tris-HCl pH 7.5, 150 mM NaCl, 0.5% tritonX-100, 10% glycerol, 10 mM NaF and a protease inhibitor cocktail. Protein concentration is determined using a BCA protein assay reagent. Cell lysates (35 μg) are separated on 7.5% or 12.5% SDS-PAGE polyacrylamide gels and transferred to PVDF membrane filters. Membranes are blocked in 5% non-fat milk in TBS containing 0.1% Tween 20. Blots are probed with antibodies to ROCK1, ROCK2 or actin and washed well before incubation with HRP-conjugated secondary antibodies and visualization with an enhanced chemiluminescence (ECL) kit.

Synonyms	KD025, Rezurock, ROCK inhibitor, SLx-2119
Molecular Weight	452.51
Formula	C26H24N6O2
CAS No.	911417-87-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 83 mg/mL (183.4 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

References and Literature

1. Lee JH, et al. Ann Clin Transl Neurol. 2014, 1(1), 2-14. 2. Zanin-Zhorov A, et al. Proc Natl Acad Sci U S A. 2014, 111(47), 16814-16819. 3. Flynn R, et al. Blood. 2016. pii: blood-2015-10-678706.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Inhibitor Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Drug Repurposing Compound Library TGF-beta/Smad Compound Library FDA-Approved Kinase Inhibitor Library Bioactive Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Belumosudil 911417-87-3 Cell Cycle/Checkpoint Cytoskeletal Signaling Stem Cells ROCK inhibit KD 025 Rho-kinase Rho-associated protein kinase ROCK2 KD025 Anti-fibrotic SLx 2119 ROK Rezurock ROCK inhibitor SLx2119 SLx-2119 Rho-associated kinase KD-025 Inhibitor inhibitor

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