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

Belumosudil (KD025) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 μM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.

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No. CAS : 911417-87-3

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10 mM * 1 mL in DMSO
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Revisión del cliente

Based on 34 publication(s) in Google Scholar

Other Forms of Belumosudil:

Belumosudil Related Antibodies

Top Publications Citing Use of Products

34 Publications Citing Use of MCE Belumosudil

WB

    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.

    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.

    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).

    Ver todos los productos específicos de isoformas ROCK:

    Ver todas las isoformas
    ROCK ROCK1 ROCK2

    • Actividad biológica

    • Protocolo

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Belumosudil (KD025) 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.

    Belumosudil Related Antibodies
    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.
    Ensayo clínico
    Peso molecular

    452.51

    Fòrmula

    C26H24N6O2
    No. CAS
    Appearance

    Solid

    Color

    Off-white to light brown

    SMILES

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

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvente y solubilidad
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2099 mL 11.0495 mL 22.0990 mL
    5 mM 0.4420 mL 2.2099 mL 4.4198 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, 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.

    • Calculadora de molaridad

    • Calculadora de dilución

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 3.33 mg/mL (7.36 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 10 mg/mL (22.10 mM); Suspended solution; Need ultrasonic

    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.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Pureza y Documentación

    Purity: 99.83%

    SDS (393 KB)

    COA (250 KB) LCMS (93 KB)

    Instrucciones de manejo (2659 KB)
    Referencias
    Ensayo celular
    [1]

    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.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Administraciòn de animales
    [2]

    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.

    MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
    Referencias

    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
    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
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    Belumosudil Related Classifications

    Help & FAQs
    • 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.

    Keywords:

    Belumosudil911417-87-3KD025 SLx-2119KD 025KD-025SLx2119SLx 2119SLx-2119ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK2Anti-fibroticInhibitorinhibitorinhibit

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    Nombre del producto:
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    Cat. No.:
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