1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK
  3. SLx-2119

SLx-2119 (Synonyms: KD-025)

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

SLx-2119 (KD-025) is a selective inhibitor of ROCK2 with an IC50 of 105 nM.

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
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500 mg   Get quote  

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Customer Review

Based on 17 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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.

    SLx-2119 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

    SLx-2119 (KD-025) is a selective inhibitor of ROCK2 with an IC50 of 105 nM.

    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

    SLx-2119 (KD-025; 100, 200 or 300 mg/kg, i.p.) dose-dependently reduces infarct volume after transient middle cerebral artery occlusion. SLx-2119 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: 2.5 mg/mL (5.52 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: 2.5 mg/mL (5.52 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: ≥ 2.5 mg/mL (5.52 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 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 SLx-2119 (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

    Purity: 99.59%

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    SLx-2119
    Cat. No.:
    HY-15307
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