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

SLx-2119 (Synonyms: ROCK inhibitor; KD-025)

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

SLx-2119 is a selective inhibitor of ROCK2 with IC50 of 105 nM, more than 200 fold selecivity over ROCK1 (IC50=24 μM).

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

SLx-2119 Chemical Structure

SLx-2119 Chemical Structure

CAS No. : 911417-87-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 114 In-stock
Estimated Time of Arrival: December 31
50 mg USD 348 In-stock
Estimated Time of Arrival: December 31
100 mg USD 588 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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    SLx-2119 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.

    SLx-2119 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    SLx-2119 is a selective inhibitor of ROCK2 with IC50 of 105 nM, more than 200 fold selecivity over ROCK1 (IC50=24 μM).

    IC50 & Target[1]

    ROCK2

    105 nM (IC50)

    ROCK1

    24 μM (IC50)

    In Vitro

    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 SLx-2119, shows a 5-times higher background than the other arrays[1].

    In Vivo

    KD025 (100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. KD025 is at least as efficacious in aged, diabetic or female mice, as in normal adult males[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 29 mg/mL (64.09 mM)

    *"≥" 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.

      Slx-2119 is prepared in vehicle (0.4% methylcellulose)[3].

    • 2.

      SLX-2119 is given in drinking water[4].

    References
    Kinase Assay
    [1]

    Cell-free enzyme assays are performed to determine the selective inhibition of ROCK1 and ROCK2 by SLx-2119. Reactions are performed on non-binding surface microplates. Four mU of human ROCK1 and ROCK2 are used to phosphorylate 30 µM of the synthetic ROCK peptide substrate S6 Long, prepared at American Peptide with the addition of 10 µM ATP, containing 33P-ATP in the presence of 10 mM Mg2+, 50 mM Tris, pH 7.5, 0.1 mM EGTA and 1 mM DTT at room temperature. One unit is the amount of kinase needed to catalyze the transfer of 1 nmol phosphate/min to the peptide. The reactions are allowed to proceed for 45 minutes and then stopped with 3% phosphoric acid to a final concentration of 1%. The reactions are captured on phospho cellulose filtration microplates and washed with 75 mM phosphoric acid and methanol using a vacuum manifold. Phosphorylation is measured on a Perkin-Elmer MicroBeta 1450.

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

    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 SLx-2119. 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 KD025 (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. Atorvastatin (4 mg/mL) is dissolved in phosphate-buffered saline (pH 7.4) containing 45% 3-hydroxypropyl-B-cyclodextrin and 10% ethanol, and administered at a dose of 20 mg/kg per day as a single daily intraperitoneal injection for 2 weeks..

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

    References
    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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.59%

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    Product Name:
    SLx-2119
    Cat. No.:
    HY-15307
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    SLx-2119

    Cat. No.: HY-15307