1. Cytoskeleton Autophagy Apoptosis
  2. Integrin Autophagy Apoptosis
  3. OSU-T315

OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain). OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner. OSU-T315 causes cell death through apoptosis and autophagy.

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OSU-T315 Chemical Structure

OSU-T315 Chemical Structure

CAS No. : 2070015-22-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    OSU-T315 purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2020 Aug;123(4):542-555.  [Abstract]

    The combination of the ILK inhibitor OSU-T315 with AKT inhibitors of either class potentiated cell death in MDA-MB-361 cells

    OSU-T315 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2019 May;110(5):1804-1813.  [Abstract]

    Effect of OSU-T315 on the proportion of ALDH-hi cells (left and middle) and the ALDH1A1 and SDPR protein level in EV HEC-108 cells (right). Equal protein loading is confirmed by quantifying β-actin (input control).
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    Description

    OSU-T315 (ILK-IN-1) is a small Integrin-linked kinase (ILK) inhibitor with an IC50 of 0.6 μM, inhibiting PI3K/AKT signaling by dephosphorylation of AKT-Ser473 and other ILK targets (GSK-3β and myosin light chain)[1]. OSU-T315 abrogates AKT activation by impeding AKT localization in lipid rafts and triggers caspase-dependent apoptosis in an ILK-independent manner[2]. OSU-T315 causes cell death through apoptosis and autophagy[1].

    IC50 & Target

    IC50: 0.6μM; Integrin-linked kinase (ILK) inhibitor[1]

    In Vitro

    OSU-T315 (Compound 22; 0-5 μM; 24 hours) exhibits high in vitro potency against a panel of prostate and breast cancer cell lines with a IC50 range of 1-2.5 μM[1].
    ? OSU-T315 (0-2.5 μM; 24 hours) can reduce YB-1, HER2, and EGFR expression; shows a modest suppressive effect on phosphorylated S6 levels, exhibits dose-dependent suppressive effects on the levels of phospho-ERK1/2 and phospho-p38, while that of phospho-JNK remains unaltered in PC-3 cell[1].
    ? OSU-T315 (0-4 μM; 24 hours) causes autophagy through ILK inhibition[1].

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

    Western Blot Analysis [1]

    Cell Line: PC-3 cells; MDA-MB-231 cells
    Concentration: 1 μM, 2 μM, 3 μM, 4 μM; 0.5 μM, 1 μM, 1.5 μM, 2 μM, 2.5 μM
    Incubation Time: 24 hours
    Result: Exhibited a dose-dependent decreasing effect on the phosphorylation of pS6, ERKs, and p38 in PC-3 cells and MDA-MB-231 cells.

    Cell Viability Assay [1]

    Cell Line: Prostate cancer cells: LNCaP, PC-3; breast cancer cells: MDA-MB-231, MDA-MB-468, SKBR3, MCF-7; PrEC and MEC cells
    Concentration: 0-5 μM
    Incubation Time: 24 hours
    Result: Suppressed cancer cells viability in breast and prostate cancer cells (IC (50), 1-2.5μM).

    Apoptosis Analysis[1]

    Cell Line: PC-3 cells
    Concentration: 1 μM, 2 μM, 3 μM, 4 μM
    Incubation Time: 24 hours
    Result: Induced accumulation of LC3-II and PARP cleavage.
    In Vivo

    OSU-T315 (Oral gavage; 25 mg/kg, 50 mg/kg; single daily; 35 days) has a suppressive effect of on PC-3 xenograft tumor growth [1].
    ? No other obvious toxicity is observed in mice[1].

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

    Animal Model: Male NCr athymic nude mice with PC-3 tumor xenografts
    Dosage: 25 mg/kg; 50 mg/kg
    Administration: Oral gavage; single daily; 35 days
    Result: Resulted in suppression of tumor growth relative to the vehicle control after 35 days of treatment (48% and 62% suppression for 25 and 50 mg/kg, respectively).
    Molecular Weight

    533.59

    Formula

    C30H30F3N5O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC)CCC1=CC(C2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)=NN1C4=CC=C(N5CCNCC5)C=C4

    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 : ≥ 260 mg/mL (487.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8741 mL 9.3705 mL 18.7410 mL
    5 mM 0.3748 mL 1.8741 mL 3.7482 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.

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    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

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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: ≥ 2.17 mg/mL (4.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (4.07 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). 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 (21.7 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: 99.88%

    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 1.8741 mL 9.3705 mL 18.7410 mL 46.8524 mL
    5 mM 0.3748 mL 1.8741 mL 3.7482 mL 9.3705 mL
    10 mM 0.1874 mL 0.9370 mL 1.8741 mL 4.6852 mL
    15 mM 0.1249 mL 0.6247 mL 1.2494 mL 3.1235 mL
    20 mM 0.0937 mL 0.4685 mL 0.9370 mL 2.3426 mL
    25 mM 0.0750 mL 0.3748 mL 0.7496 mL 1.8741 mL
    30 mM 0.0625 mL 0.3123 mL 0.6247 mL 1.5617 mL
    40 mM 0.0469 mL 0.2343 mL 0.4685 mL 1.1713 mL
    50 mM 0.0375 mL 0.1874 mL 0.3748 mL 0.9370 mL
    60 mM 0.0312 mL 0.1562 mL 0.3123 mL 0.7809 mL
    80 mM 0.0234 mL 0.1171 mL 0.2343 mL 0.5857 mL
    100 mM 0.0187 mL 0.0937 mL 0.1874 mL 0.4685 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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