Belumosudil
Based on 34 publication(s) in Google Scholar
Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.83%
- No. CAS: 911417-87-3
- Fòrmula: C26H24N6O2
- Peso molecular:452.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Belumosudil
More- J Adv Res. 2024 Jul 5:S2090-1232(24)00269-8. [Abstract]
- J Autoimmun. 2018 May:89:125-138. [Abstract]
- Fundam Res. 2025 Sep 24.
- Biochem Pharmacol. 2025 Oct 23:117451. [Abstract]
- Biochem Pharmacol. 2025 Apr 8:116933. [Abstract]
- Neurobiol Dis. 2019 Apr;124:520-530. [Abstract]
- Am J Respir Cell Mol Biol. 2020 Oct;63(4):519-530. [Abstract]
- Int Immunopharmacol. 2023 May:118:110017. [Abstract]
- Molecules. 2020 Mar 17;25(6):1369. [Abstract]
- Am J Physiol Heart Circ Physiol. 2022 Jul 1;323(1):H235-H247. [Abstract]
- Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]
- J Proteome Res. 2025 Oct 3;24(10):4935-4951. [Abstract]
- Heliyon. 2024 Sep 24;10(19):e38369. [Abstract]
- Adipocyte. 2019 Dec;8(1):114-124. [Abstract]
- Curr Issues Mol Biol. 2025 Jul 3;47(7):513. [Abstract]
- PLoS One. 2017 May 16;12(5):e0177332. [Abstract]
- Curr Eye Res. 2025 Jun 2:1-11. [Abstract]
- Acta Chromatogr. 2025 Feb 25.
- JCI Insight. 2018 Jun 7;3(11). pii: 98921. [Abstract]
- Acta Crystallogr F Struct Biol Commun. 2022 Oct 1;78(Pt 10):348-353. [Abstract]
- Res Sq. 2026 Mar 8.
- bioRxiv. 2025 Jul 25.
- bioRxiv. 2025 April 25.
- bioRxiv. 2024 September 21.
- bioRxiv. 2023 Jul 21:2023.07.19.549794. [Abstract]
- SSRN. 2022 Nov 21.
- Patent. US20190298733A1.
- Patent. US9937154B2.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
- Patent. US9687483B2.
- Patent. US20160361300A1.
- Patent. US20160346224A1.
- University Goettingen. 2016 Oct.
- Patent. US20160213664A1.
Customer Validation & Images
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WB
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Actividad biológica
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ROCK2 105 nM (IC50) |
ROCK1 24 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 911417-87-3
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Appearance Solid
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Peso molecular 452.51
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Fòrmula C26H24N6O2
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Color Off-white to light brown
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SMILES
O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1
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Synonyms
KD025; SLx-2119
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (34)
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Journal Impact Factor
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Most Recent
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J Adv Res
2024 Jul 5:S2090-1232(24)00269-8. PMID: 38972542 -
J Autoimmun
Critical role of ROCK2 activity in facilitating mucosal CD4+ T cell activation in inflammatory bowel disease. [Abstract]2018 May:89:125-138. PMID: 29269245
Belumosudil purchased from MedChemExpress. Usage Cited in: J Autoimmun. 2018 May:89:125-138. [Abstract]
Cells are collected on day 2 for analysis of phosphorylation of Stat1, Stat3, and Stat5 using western blots.
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Biochem Pharmacol
2025 Oct 23:117451. PMID: 41138926 -
Biochem Pharmacol
The dual targeting effects of KD025 on casein kinase 2 and ROCK2 in a mouse model of diet-induced obesity. [Abstract]2025 Apr 8:116933. PMID: 40210126 -
Neurobiol Dis
Rho-kinase inhibition has antidepressant-like efficacy and expedites dendritic spine pruning in adolescent mice. [Abstract]2019 Apr;124:520-530. PMID: 30593834 -
Am J Respir Cell Mol Biol
KD025 Shifts Pulmonary Endothelial Cell Bioenergetics and Decreases Baseline Lung Permeability. [Abstract]2020 Oct;63(4):519-530. PMID: 32628869 -
Int Immunopharmacol
Comparative transcriptome profile of mouse macrophages treated with the RhoA/Rock pathway inhibitors Y27632, Fingolimod (Gilenya), and Rezurock (Belumosudil, SLx-2119). [Abstract]2023 May:118:110017. PMID: 36931169 -
Molecules
Determination of KD025 (SLx-2119), a Selective ROCK2 Inhibitor, in Rat Plasma by High-Performance Liquid Chromatography-Tandem Mass Spectrometry and its Pharmacokinetic Application. [Abstract]2020 Mar 17;25(6):1369. PMID: 32192179 -
Am J Physiol Heart Circ Physiol
Belumosudil, ROCK2-specific inhibitor, alleviates cardiac fibrosis by inhibiting cardiac fibroblasts activation. [Abstract]2022 Jul 1;323(1):H235-H247. PMID: 35657612 -
Sci Rep
Anti-adipogenic effects of KD025 (SLx-2119), a ROCK2-specific inhibitor, in 3T3-L1 cells. [Abstract]2018 Feb 6;8(1):2477. PMID: 29410516
Belumosudil purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477. [Abstract]
Cells lysates are subjected to SDS-PAGE and immunoblotted with anti-phospho-Akt (Ser473) and total Akt antibodies. PPARγ is used as a differentiation marker, and β-tubulin and α-actin as loading controls.
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J Proteome Res
Molecular Profiling of Belumosudil-Treated IOMM-Lee Meningioma Cells Reveals Repurposing Potential via Enhanced Oxidative Phosphorylation and ROS-Mediated Cell Death. [Abstract]2025 Oct 3;24(10):4935-4951. PMID: 40944662 -
Heliyon
Comprehensive chromatographic analysis of Belumosudil and its degradation products: Development, validation, and In silico toxicity assessment. [Abstract]2024 Sep 24;10(19):e38369. PMID: 39391480 -
Adipocyte
KD025 (SLx-2119) suppresses adipogenesis at intermediate stage in human adipose-derived stem cells. [Abstract]2019 Dec;8(1):114-124. PMID: 30860936 -
Curr Issues Mol Biol
Total Flavones of Rhododendron Protect Against Ischemic Cerebral Injury by Regulating the Phosphorylation of the RhoA-ROCK2 Pathway via Endothelial-Derived H2S. [Abstract]2025 Jul 3;47(7):513. PMID: 40728982 -
PLoS One
Selective inhibition of brain endothelial Rho-kinase-2 provides optimal protection of an in vitro blood-brain barrier from tissue-type plasminogen activator and plasmin. [Abstract]2017 May 16;12(5):e0177332. PMID: 28510599 -
Curr Eye Res
Therapeutic Effects and Molecular Mechanisms of KD025 in Intraocular Pressure Regulation. [Abstract]2025 Jun 2:1-11. PMID: 40452331 -
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JCI Insight
Repurposing sertraline sensitizes non-small cell lung cancer cells to erlotinib by inducing autophagy. [Abstract]2018 Jun 7;3(11). pii: 98921. PMID: 29875309 -
Acta Crystallogr F Struct Biol Commun
Crystal structure of the Rho-associated coiled-coil kinase 2 inhibitor belumosudil bound to CK2α. [Abstract]2022 Oct 1;78(Pt 10):348-353. PMID: 36189718 -
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bioRxiv
Modeling Mechanical Activation of Macrophages During Pulmonary Fibrogenesis for Targeted Anti-Fibrosis Therapy. [Abstract]2023 Jul 21:2023.07.19.549794. PMID: 37503121 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898 -
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Belumosudil purchased from MedChemExpress. Usage Cited in: University Goettingen. 2016 Oct.
Purified ROCK1 and ROCK2 are incubated with H1152P (3 µM) or SLx-2119 (3 µM) prior to performing the in vitro kinase assay. Shown is a representative autoradiography (n=3).
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Solvente y solubilidad
DMSO : 23.33 mg/mL (51.56 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)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 3.33 mg/mL (7.36 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 10 mg/mL (22.10 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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 Belumosudil. 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Young adult (C57BL/6, 2-3 months old, male 22-30 g, female 16-23 g), aged (C57BL/6, 12 months old, 33-52 g) are used in all experiments. Vehicle (0.4% methylcellulose) or Belumosudil (100, 200 or 300 mg/kg) is administered every 12 h via orogastric gavage. The dosing paradigm is chosen based on the pharmacokinetic profile after oral administration in mice.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[2]. Lee, J.H., et al. Selective ROCK2 Inhibition In Focal Cerebral Ischemia. Ann Clin Transl Neurol. 2014 Jan 1;1(1):2-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.2099 mL | 11.0495 mL | 22.0990 mL | 55.2474 mL |
| 5 mM | 0.4420 mL | 2.2099 mL | 4.4198 mL | 11.0495 mL | |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2099 mL | 5.5247 mL | |
| 15 mM | 0.1473 mL | 0.7366 mL | 1.4733 mL | 3.6832 mL | |
| 20 mM | 0.1105 mL | 0.5525 mL | 1.1049 mL | 2.7624 mL | |
| 25 mM | 0.0884 mL | 0.4420 mL | 0.8840 mL | 2.2099 mL | |
| 30 mM | 0.0737 mL | 0.3683 mL | 0.7366 mL | 1.8416 mL | |
| 40 mM | 0.0552 mL | 0.2762 mL | 0.5525 mL | 1.3812 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4420 mL | 1.1049 mL |
Belumosudil Related Classifications
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