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

Belumosudil (Synonyms: KD025; SLx-2119)

Cat. No.: HY-15307 Purity: 99.59%
Handling Instructions

Belumosudil (KD025) 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 Chemical Structure

Belumosudil Chemical Structure

CAS No. : 911417-87-3

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10 mM * 1 mL in DMSO USD 92 In-stock
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5 mg USD 84 In-stock
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10 mg USD 114 In-stock
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50 mg USD 348 In-stock
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100 mg USD 588 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Belumosudil purchased from MCE. Usage Cited in: J Autoimmun. 2018 May;89:125-138.

    Cells are collected on day 2 for analysis of phosphorylation of Stat1, Stat3, and Stat5 using western blots.

    Belumosudil purchased from MCE. Usage Cited in: Sci Rep. 2018 Feb 6;8(1):2477.

    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 MCE. 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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    • Protocol

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    Description

    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].

    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].

    Clinical Trial
    Molecular Weight

    452.51

    Formula

    C₂₆H₂₄N₆O₂

    CAS No.

    911417-87-3

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 29 mg/mL (64.09 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.2210 mL 1.1049 mL 2.2099 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.08 mg/mL (4.60 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    References

    Purity: 99.59%

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    Keywords:

    BelumosudilKD025SLx-2119KD 025KD-025SLx2119SLx 2119ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKROCK2Anti-fibroticInhibitorinhibitorinhibit

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    Product Name:
    Belumosudil
    Cat. No.:
    HY-15307
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