Belumosudil mesylate (Synonyms: KD025 mesylate; SLx-2119 mesylate) |
| Catalog No.GC26330 |
Belumosudil mesylate is a selective ROCK2 inhibitor, with IC50 values of 105nM for ROCK2 and 24µM for ROCK1.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2109704-99-4
Sample solution is provided at 25 µL, 10mM.
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Belumosudil mesylate is a selective ROCK2 inhibitor, with IC50 values of 105nM for ROCK2 and 24µM for ROCK1[1]. ROCK2 is a critical regulator of immune modulation and fibrosis[2].The selective inhibitor of ROCK2 belumosudil mesylate can reduces fibrosis by downregulating both transforming growth factor-β signaling and profibrotic gene expression and usually be utilized in research on chronic graft-versus-host disease (cGVHD)[3][4]. Additionally, belumosudil mesylate can also be used for research in other immune-related diseases such as systemic sclerosisue to its anti-inflammatory and antifibrotic activities[5].
In vitro, treatment of cardiac fibroblasts(CFs) with different concentrations of belumosudil mesylate (0.625, 1.25, 2.5 and 5μM) for 24h after serum starvation for 24h selectively inhibits ROCK2 and reduces the phosphorylation of Smad2 in a dose-dependent manner[6]. Treatment of PASMC cells with belumosudil mesylate ( 40µM; 24h) induces significant down-regulations of Tsp-1 and CTGF mRNA levels[1].
In vivo, belumosudil mesylate(100, 200 or 300mg/kg) was administered every 12h via orogastric gavage for a total of five doses to young adult (C57BL/6, 2–3 months old, male 22–30g, female 16–23g), aged (C57BL/6, 12 months old, 33–52g), or type 2 diabetic mice，it dose-dependently reduces infarct volume after transient middle cerebral artery occlusion,and it is at least as efficacious in aged, diabetic or female mice, as in normal adult males[7].
References:
[1] Boerma, M., Fu, Q., Wang, J., Loose, D. S., Bartolozzi, A., Ellis, J. L., McGonigle, S., Paradise, E., Sweetnam, P., Fink, L. M., Vozenin-Brotons, M. C., & Hauer-Jensen, M. (2008). Comparative gene expression profiling in three primary human cell lines after treatment with a novel inhibitor of Rho kinase or atorvastatin. Blood coagulation & fibrinolysis : an international journal in haemostasis and thrombosis, 19(7), 709–718.
[2] Zanin-Zhorov, A., & Blazar, B. R. (2021). ROCK2, a critical regulator of immune modulation and fibrosis has emerged as a therapeutic target in chronic graft-versus-host disease. Clinical immunology (Orlando, Fla.), 230, 108823.
[3] N., Toyosaki, M., Katayama, Y., Murayama, S., Sasagawa, Y., Maeda, Y., Hatake, K., & Teshima, T. (2024). An open-label study of belumosudil, a selective ROCK2 inhibitor, as second or subsequent line of therapy for steroid-dependent/steroid-resistant chronic GVHD. American journal of hematology, 99(10), 1917–1926.
[4] Taylor, B., Cohen, J., Tejeda, J., & Wang, T. P. (2022). Belumosudil for chronic graft-versus-host disease. Drugs of today (Barcelona, Spain : 1998), 58(5), 203–212.
[5] Gunes, I., Bernstein, E., Cowper, S. E., Panse, G., Pradhan, N., Camacho, L. D., Page, N., Bundschuh, E., Williams, A., Carns, M., Aren, K., Fantus, S., Volkmann, E. R., Bukiri, H., Correia, C., Wang, R., Kolachalama, V., Wilson, F. P., Mawe, S., Mahoney, J. M., … Hinchcliff, M. (2024). Neural network analysis as a novel skin outcome in a trial of belumosudil in patients with systemic sclerosis. Research square, rs.3.rs-4889334.
[6] Liu, Q., Li, H. Y., Wang, S. J., Huang, S. Q., Yue, Y., Maihemuti, A., Zhang, Y., Huang, L., Luo, L., Feng, K. N., & Wu, Z. K. (2022). Belumosudil, ROCK2-specific inhibitor, alleviates cardiac fibrosis by inhibiting cardiac fibroblasts activation. American journal of physiology. Heart and circulatory physiology, 323(1), H235–H247.
[7] Lee, J. H., Zheng, Y., von Bornstadt, D., Wei, Y., Balcioglu, A., Daneshmand, A., Yalcin, N., Yu, E., Herisson, F., Atalay, Y. B., Kim, M. H., Ahn, Y. J., Balkaya, M., Sweetnam, P., Schueller, O., Poyurovsky, M. V., Kim, H. H., Lo, E. H., Furie, K. L., & Ayata, C. (2014). Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Annals of clinical and translational neurology, 1(1), 2–14.
| Cell experiment [1]: | |
Cell lines | Cardiac fibroblasts(CFs) |
Preparation Method | Tissue culture plastic was used as the experimental platform. Adult CFs were cultured in DMEM containing 10% FBS, 100U/mL penicillin, and 100μg/mL streptomycin with media changed every other day. When nearly confluence, CFs were trypsinized and sub-cultured at 1:3 ratio. CFs were serum-starved for 24h before TGF-β1 treatment (10ng/ml) with or without different concentrations of belumosudil mesylate (0.625, 1.25, 2.5 and 5μM) for 24h. Proteins were extracted for western blot analysis. |
Reaction Conditions | 0.625, 1.25, 2.5 and 5μM; 24h |
Applications | Belumosudil mesylate selectively inhibits ROCK2 and reduces the phosphorylation of Smad2 in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Young adult (C57BL/6, 2–3 months old, male 22–30g, female 16–23g), aged (C57BL/6, 12 months old, 33–52g), or type 2 diabetic mice (db/db, B6.BKS(D)-Lepr db/J, Jackson Laboratory; 2–3 months old, male, 33–50g) |
Preparation Method | Animals received 100, 200 or 300mg/kg belumosudil mesylate twice a day for a total of five doses via orogastric gavage. fMCAO was induced in mice under isoflurane anesthesia (2.5% induction, 1.2% maintenance, in 70% N2O/30% O2). At 48h after fMCAO, infarct areas were measured on ten 1 mm-thick 2,3,5-triphenyltetrazolium chloride (TTC)-stained coronal sections, integrated to calculate the infarct volume, and corrected for ischemic edema by subtracting the volume of ipsilateral non-infarcted tissue from the contralateral hemisphere. |
Dosage form | 100, 200 or 300 mg/kg; i.g. |
Applications | Belumosudil mesylate dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. |
References: | |
| Cas No. | 2109704-99-4 | SDF | |
| Synonyms | KD025 mesylate; SLx-2119 mesylate | ||
| Formula | C27H28N6O5S | M.Wt | 548.61 |
| Solubility | DMSO : 12.5 mg/mL (22.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) | Storage | 4°C, sealed storage, away from moisture |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.8228 mL | 9.1139 mL | 18.2279 mL |
| 5 mM | 0.3646 mL | 1.8228 mL | 3.6456 mL |
| 10 mM | 0.1823 mL | 0.9114 mL | 1.8228 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
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.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Quality Control & SDS
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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