1. Protein Tyrosine Kinase/RTK
  2. FAK
  3. ZINC40099027

ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research.

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

CAS No. : 1211825-25-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
WB
Cell Imaging/Staining
Bio/Physico-chemical Assay

    ZINC40099027 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 5:225:856-870.  [Abstract]

    ZINC40099027 (10 nM; 2 h) significantly reversed the suppression of FAK and ERK phosphorylation induced by DUSP26 overexpression in H9c2 cells exposed to GP. β-actin.

    ZINC40099027 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 5:225:856-870.  [Abstract]

    ZINC40099027 (10 nM; 2 h) treatment led to significant changes in mitochondrial ROS and membrane potential in H9c2 cells, as evidenced by MitoSOX and JC-1 staining.

    ZINC40099027 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 5:225:856-870.  [Abstract]

    ZINC40099027 (10 nM; 2 h), a potent FAK activator, altered basal respiration, ATP production, and maximal respiration in DUSP26-overexpressing H9c2 cells.

    ZINC40099027 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 5:225:856-870.  [Abstract]

    ZINC40099027 (10 nM; 2 h) reversed the changes of mitochondrial dynamic proteins (Drp1, Mfn1, Mfn2, and OPA1) in H9c2 cells induced by DUSP26 overexpression.

    ZINC40099027 purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2024 Nov 5:225:856-870.  [Abstract]

    FAK activator ZINC40099027 (10 nM; 2 h) caused a significant increase in lipid droplet accumulation in DUSP26-overexpressing H9c2 cells under glucolipotoxic conditions.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    ZINC40099027 is a selective FAK activator. ZINC40099027 promotes FAK phosphorylation, without activating its paralogs Pyk2 and Src. ZINC40099027 promotes the wound closure of human intestinal epithelial monolayers and the healing of mouse ulcers by activating FAK. ZINC40099027 can be used for diseases related to gastrointestinal mucosal injury research[1].

    In Vitro

    ZINC40099027 (10-1000 nM, 1 h) promotes FAK phosphorylation in Caco-2 intestinal epithelial cells[1].
    ZINC40099027 (10 nM; 24 hours) accelerates the wound closure of Caco-2 epithelial monolayers[1].

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

    Western Blot Analysis[1]

    Cell Line: Caco-2 intestinal epithelial cells
    Concentration: 10 nM, 100 nM, 1000 nM
    Incubation Time: 1 h
    Result: Specifically increased FAK-Tyr 397 phosphorylation within intact cells while activating neither Pyk2, a close paralogue of FAK, nor Src, another key nonreceptor kinase within the focal adhesion complex.
    In Vivo

    ZINC40099027 (900 µg/kg; intraperitoneal injection; once every 6 hours; treatment for 3 days) promotes intestinal mucosal healing, reduces the ulcer area, increases the immunoreactivity of phosphorylated FAK in the epithelium at the edge of the ulcer, and does not affect the percentage of Ki-67 positive cells in the Acetic acid (HY-Y0319)-induced ischemic ulcer model in mice[1].
    ZINC40099027 (900 µg/kg; intraperitoneal injection; once every 6 hours; treatment for 3 days) promotes ulcer healing, reduces the total ulcer area, and has no significant effect on the morphology of the kidneys and liver in the Indomethacin (HY-14397)-induced small intestine injury model in mice[1].

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

    Animal Model: C57BL/6J mice (both male and female, 8-10 weeks old), the ischemic ulcer model was induced by placing a 75% Acetic acid-saturated circular filter disk on the antimesenteric serosa of the jejunum for 15 seconds[1]
    Dosage: 900 µg/kg
    Administration: Intraperitoneal injection, once every 6 hours, for 3 days
    Result: Had smaller ulcers than those receiving the DMSO control.
    The percentage of wound closure was markedly higher.
    Showed higher immunoreactivity for phosphorylated FAK in the epithelium at the edge.
    Animal Model: C57BL/6J mice (both male and female, 8-10 weeks old), the Indomethacin-induced ulcer model was induced by subcutaneous injection of 15 mg/kg Indomethacin dissolved in 100% ethanol[1]
    Dosage: 900 µg/kg
    Administration: Intraperitoneal injection, once every 6 hours, for 3 days
    Result: Reduced the total ulcer area compared to the DMSO control.
    Molecular Weight

    449.47

    Formula

    C23H26F3N3O3

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1C(C2=CC=C(OC)C=C2)CCC1)NC3=CC(C(F)(F)F)=CC=C3N4CCOCC4

    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 : 100 mg/mL (222.48 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 2.2248 mL 11.1242 mL 22.2484 mL
    5 mM 0.4450 mL 2.2248 mL 4.4497 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% Corn Oil

      Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
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    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: 99.97%

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2248 mL 11.1242 mL 22.2484 mL 55.6211 mL
    5 mM 0.4450 mL 2.2248 mL 4.4497 mL 11.1242 mL
    10 mM 0.2225 mL 1.1124 mL 2.2248 mL 5.5621 mL
    15 mM 0.1483 mL 0.7416 mL 1.4832 mL 3.7081 mL
    20 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7811 mL
    25 mM 0.0890 mL 0.4450 mL 0.8899 mL 2.2248 mL
    30 mM 0.0742 mL 0.3708 mL 0.7416 mL 1.8540 mL
    40 mM 0.0556 mL 0.2781 mL 0.5562 mL 1.3905 mL
    50 mM 0.0445 mL 0.2225 mL 0.4450 mL 1.1124 mL
    60 mM 0.0371 mL 0.1854 mL 0.3708 mL 0.9270 mL
    80 mM 0.0278 mL 0.1391 mL 0.2781 mL 0.6953 mL
    100 mM 0.0222 mL 0.1112 mL 0.2225 mL 0.5562 mL
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    • 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:
    ZINC40099027
    Cat. No.:
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