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SLx-2119 (Synonyms: Belumosudil, SLx-2119)

Catalog No.GC12827

A ROCK2 inhibitor

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SLx-2119 Chemical Structure

Cas No.: 911417-87-3

Size Price Stock Qty
10mM (in 1mL DMSO)
$123.00
In stock
5mg
$76.00
In stock
10mg
$103.00
In stock
25mg
$239.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Inhibitory activities

Cell-free enzyme assays were performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions were performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 were used to phosphorylate 30 μM of the synthetic ROCK peptide substrate S6 Long (sequence: KEAKEKRQEQIAKRRRLSSLRASTSKSGGSQK), prepared at American Peptide (Sunnyvale, CA) 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 were allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions were captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation was measured on a Perkin-Elmer MicroBeta 1450.

Cell experiment [1]:

Cell lines

Human microvascular endothelial cells (HMVEC; CC-2527, Cambrex).

Preparation method

Dissolved in DMSO to obtain a stock solution of 20 mM [1]. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

3 ml culture media containing 10 μM or 40 μM SLx-2119; 24 h.

Applications

SLx-2119 at 40 μM significantly reduces the mRNA levels of Tsp-1 and CTGF.

Animal experiment [2]:

Animal models

C57BL/6 mice.

Dosage form

100, 200 or 300 mg/kg; administered every 12 h for 2 days via orogastric gavage.

Applications

KD025 (formerly SLx-2119) reduces infarct volume by 30% and 40% at 100 and 200 mg/kg dose levels. KD025 (200 mg/kg 90 min before distal middle cerebral artery occlusion (dMCAO)) significantly reduces the area of perfusion defect, suggesting that ROCK2 inhibition improves cortical perfusion during acute cerebral arterial occlusion.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[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, 2008, 19(7): 709-718.

[2]. Lee JH, Zheng Y, von Bornstadt D, et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol, 2014, 1(1): 2-14.

Background

SLx-2119(KD-025) is a selective inhibitor of ROCK2 with IC50 of 105 nM [1].
Rho-associated protein kinase (ROCK) is a serine-threonine kinase and is involved in regulating cytoskeletal dynamics. It is associated with many intracellular processes, which are relevant to stroke. ROCK2 is the predominant isoform mainly expressed in vasculature and neurons [2].
In smooth muscle cells isolated from human intestine with radiation-induced fibrosis (RE-SMC), SLx-2119 reduced mRNA level of CTGF. Over-expression of which is associated with fibrotic diseases. While, in SMC isolated from normal human intestine (N-SMC), SLx-2119 didn't change CTGF mRNA level [1].
In focal cerebral ischemia mice, after transient middle cerebral artery occlusion, KD025 reduced infarct volume in a dose-dependant way. And the efficacy maintained for at least 4 weeks. In aged male and female mice, as well as in type 2 diabetes mice, KD025 reduced infarct volume by 34%, 42% and 32% in aged male mice, female mice and diabetic mice respectively compared to vehicle in mice [2].
References:
[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, 2008, 19(7): 709-718.
[2]. Lee JH, Zheng Y, von Bornstadt D, et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol, 2014, 1(1): 2-14.

Chemical Properties

Cas No. 911417-87-3 SDF
Synonyms Belumosudil, SLx-2119
Chemical Name 2-(3-(4-((1H-indazol-5-yl)amino)quinazolin-2-yl)phenoxy)-N-isopropylacetamide
Canonical SMILES O=C(C([H])([H])OC1=C([H])C([H])=C([H])C(C2=NC3=C([H])C([H])=C([H])C([H])=C3C(N([H])C(C([H])=C4[H])=C([H])C5=C4N([H])N=C5[H])=N2)=C1[H])N([H])C(C([H])([H])[H])([H])C([H])([H])[H]
Formula C26H24N6O2 M.Wt 452.51
Solubility ≥ 22.65 mg/mL in DMSO, ≥ 26.4 mg/mL in EtOH with ultrasonic and warming Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2099 mL 11.0495 mL 22.099 mL
5 mM 0.442 mL 2.2099 mL 4.4198 mL
10 mM 0.221 mL 1.1049 mL 2.2099 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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