1. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  2. ROCK
  3. Belumosudil mesylate

Belumosudil mesylate  (Synonyms: KD025 mesylate; SLx-2119 mesylate)

Cat. No.: HY-15307A Purity: 99.88%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Belumosudil mesylate Chemical Structure

Belumosudil mesylate Chemical Structure

CAS No. : 2109704-99-4

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1 mg USD 36 In-stock
5 mg USD 84 In-stock
10 mg USD 114 In-stock
25 mg USD 225 In-stock
50 mg USD 348 In-stock
100 mg USD 588 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 24 publication(s) in Google Scholar

Other Forms of Belumosudil mesylate:

Top Publications Citing Use of Products

    Belumosudil mesylate 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.

    Belumosudil mesylate 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.

    Belumosudil mesylate purchased from MedChemExpress. Usage Cited in: Medizinische Fakultät, 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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    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].

    IC50 & Target[1]

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    Molecular Weight

    548.61

    Formula

    C27H28N6O5S

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(NC(C)C)COC1=CC=CC(C2=NC(NC3=CC4=C(NN=C4)C=C3)=C5C=CC=CC5=N2)=C1.OS(=O)(C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    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.
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    Purity & Documentation
    References

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.8228 mL 9.1139 mL 18.2279 mL 45.5697 mL
    5 mM 0.3646 mL 1.8228 mL 3.6456 mL 9.1139 mL
    10 mM 0.1823 mL 0.9114 mL 1.8228 mL 4.5570 mL
    15 mM 0.1215 mL 0.6076 mL 1.2152 mL 3.0380 mL
    20 mM 0.0911 mL 0.4557 mL 0.9114 mL 2.2785 mL
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    Belumosudil mesylate Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Belumosudil mesylate
    Cat. No.:
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