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

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

Cat. No.: HY-15307A
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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Top Publications Citing Use of Products

    Belumosudil mesylate 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 mesylate 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 mesylate 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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    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].

    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].

    Molecular Weight

    548.61

    Formula

    C₂₇H₂₈N₆O₅S

    CAS No.

    2109704-99-4

    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

    Please store the product under the recommended conditions in the Certificate of Analysis.

    References
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    Keywords:

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

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    Product Name:
    Belumosudil mesylate
    Cat. No.:
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