1. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  2. ROCK
  3. LX7101

LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

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

LX7101 Chemical Structure

LX7101 Chemical Structure

CAS No. : 1192189-69-7

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 286 In-stock
Solution
10 mM * 1 mL in DMSO USD 286 In-stock
Solid
2 mg USD 100 In-stock
5 mg USD 200 In-stock
10 mg USD 350 In-stock
25 mg USD 700 In-stock
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100 mg USD 2200 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products
WB
Proliferation Assay

    LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Mar 16.  [Abstract]

    Both LX7101 (5 μM) and TH-257 (5 μM) inhibits the colony-forming ability of melanoma cells (A375-MA2, MeWo, and SK-MEL-147 cells) in soft-agar.

    LX7101 purchased from MedChemExpress. Usage Cited in: Oncogene. 2023 Mar 16.  [Abstract]

    Both LX7101 (5 μM; 24 h) and TH-257 (5 μM; 24 h) reduces the phosphorylation of G3BP1 in A375-MA2 and SK-MEL-147 cells.

    LX7101 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Aug 2;8(1):11585.  [Abstract]

    Western blot analysis of GFAP protein levels in LX7101 and DMSO-treated iNPC-KO lines. GAPDH is used as a loading control.

    View All ROCK Isoform Specific Products:

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LX7101 is a potent inhibitor of LIMK and ROCK2 with IC50 values of 24, 1.6 and 10 nM for LIMK1, LIMK2 and ROCK2, respectively; also inhibits PKA with an IC50 less than 1 nM.

    IC50 & Target[1]

    ROCK2

    10 nM (IC50)

    LIMK2

    1.6 nM (IC50)

    LIMK1

    24 nM (IC50)

    PKA

    1 nM (IC50)

    In Vitro

    LX7101 is a dual LIM-kinase and ROCK inhibitor for the treatment of ocular hypertension and associated glaucoma. LX-7101 also displays potent inhibition of Akt1 with an IC50 of less than 1 nM[1]. The overall selectivity of LX7101 for LIMK2 increases at the higher physiological ATP concentrations. Under physiological conditions, the activity of LX7101 is primarily due to inhibition of LIMK2[2].

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

    In Vivo

    LX-7101 is advanced to Phase-I clinical trials as an intraocular pressure (IOP)-lowering agent for treatment of glaucoma. LX-7101 displays a significant IOP reduction at time points ranging from 1 h to 6 h post administration in rabbits[1]. Topical doses of LX-7101 are evaluated for tolerability on the eyes of mice, rats, and rabbits. It is well tolerated at doses up to 0.5% in non-GLP single dose studies. In the mouse IOP assay, LX-7101 (5%) achieved additional reduction of IOP (5.0 mmHg total reduction) compared to the 0.1% formulation and demonstrated a long duration of action, with IOP not returning to baseline until more than 8 h postdose[2].

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

    Clinical Trial
    Molecular Weight

    451.52

    Formula

    C23H29N7O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    NCC1(C(NC2=CC(OC(N(C)C)=O)=CC=C2)=O)CCN(C3=C4C(NC=C4C)=NC=N3)CC1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 150 mg/mL (332.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2147 mL 11.0737 mL 22.1474 mL
    5 mM 0.4429 mL 2.2147 mL 4.4295 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    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: ≥ 7.5 mg/mL (16.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 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.
    • Protocol 2

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

      Solubility: ≥ 7.5 mg/mL (16.61 mM); Clear solution

      This protocol yields a clear solution of ≥ 7.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (75.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Purity & Documentation

    Purity: 99.75%

    References

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2147 mL 11.0737 mL 22.1474 mL 55.3685 mL
    5 mM 0.4429 mL 2.2147 mL 4.4295 mL 11.0737 mL
    10 mM 0.2215 mL 1.1074 mL 2.2147 mL 5.5369 mL
    15 mM 0.1476 mL 0.7382 mL 1.4765 mL 3.6912 mL
    20 mM 0.1107 mL 0.5537 mL 1.1074 mL 2.7684 mL
    25 mM 0.0886 mL 0.4429 mL 0.8859 mL 2.2147 mL
    30 mM 0.0738 mL 0.3691 mL 0.7382 mL 1.8456 mL
    40 mM 0.0554 mL 0.2768 mL 0.5537 mL 1.3842 mL
    50 mM 0.0443 mL 0.2215 mL 0.4429 mL 1.1074 mL
    60 mM 0.0369 mL 0.1846 mL 0.3691 mL 0.9228 mL
    80 mM 0.0277 mL 0.1384 mL 0.2768 mL 0.6921 mL
    100 mM 0.0221 mL 0.1107 mL 0.2215 mL 0.5537 mL
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    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.

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    Product Name:
    LX7101
    Cat. No.:
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