2. Immunology/Inflammation
  3. SphK
  4. Opaganib

Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.

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

Opaganib Chemical Structure

Opaganib Chemical Structure

CAS No. : 915385-81-8

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

Based on 9 publication(s) in Google Scholar

Other Forms of Opaganib:

Opaganib Related Antibodies

Top Publications Citing Use of Products

    Opaganib purchased from MedChemExpress. Usage Cited in: Arch Med Res. 2018 Jul;49(5):335-341.  [Abstract]

    Inhibition of SphK2 by si-RNA (si-SphK2) and ABC294640 (ABC) decrease phosphorylation and acetylation of STAT3 . Also, both si-RNA and ABC294640 reverse IL-6 induced increasing phosphorylation and acetylation of STAT3.

    Opaganib purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2018 Nov;1864(11):3824-3836.  [Abstract]

    NRK-49F cells are treated with TGF-β1 for the indicated time. The levels of p-STAT3, p-AKT, p-GSK3α, and p-GSK3β expression are detected in comparison with the levels of total STAT3, AKT, GSK3α, GSK3β, and with GAPDH as the loading control.

    Opaganib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Mar 29;7(13):16663-75.  [Abstract]

    The western blot demonstrates the effect of ABC294640 (25 μM) for 24 h in the presence and absence of MG132 (10 μM) on Des1 expression. Actin is used a protein loading control.

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    SphK1 SphK2

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Opaganib (ABC294640) is a selective, competitive sphingosine kinase 2 (SK2) inhibitor with Ki of 9.8 μM.

    IC50 & Target

    Ki: 9.8 μM (SK2)[1]
    In Vitro

    Using recombinant human SK1 and SK2, Opaganib demonstrates dose-dependent inhibition of SK2 with an IC50 of approximately 60 μM without affecting the activity of SK1 at concentrations up to at least 100 μM. In contrast, N,N-dimethylsphingosine (DMS) inhibits both SK1 and SK2 with IC50 values of approximately 60 and 20 μM, respectively. Kinetic analyses of varying concentrations of Opaganib (ABC294640) in the presence of 2.5 to 25 μM sphingosine indicated a Ki of 9.8±1.4 μM for the inhibition of SK2. Opaganib (ABC294640) decreases [3H]S1P formation in a dose-dependent fashion with an IC50 value of 26 μM[1]. IC50 values for Opaganib (ABC294640) are approximately 50 and 60 μM for A-498 and Bxpc-3 cells, respectively; whereas the IC50 values for Opaganib (ABC294640) are approximately 20 and 40 μM for these cells[2].

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

    Opaganib Related Antibodies
    In Vivo

    Opaganib induces a transient minor decrease in the hematocrit of rats. Hematology studies indicate decreases in red blood cell number and hematocrit of approximately 20% in animals given either 100 or 250 mg/kg/day; and a slight increase in neutrophils and decrease in basophils in the treated rats[1]. Mice are gavaged with Opaganib (50 mg/kg), a selective inhibitor of sphingosine kinase-2 (SK2), 1 h before surgery and subjected to 1 h-warm ischemia to ~70% of the liver followed by reperfusion. Opaganib-treatment largely prevented the increase of sphingosine-1-phosphate (S1P) after ischemia-reperfusion (IR) in vivo[2].

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

    380.91

    Formula

    C23H25ClN2O
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C1(C2)CC3(C4=CC=C(Cl)C=C4)CC2CC(C3)C1)NCC5=CC=NC=C5
    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 (262.53 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 2.6253 mL 13.1265 mL 26.2529 mL
    5 mM 0.5251 mL 2.6253 mL 5.2506 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)

    Mass
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    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

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    C2

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    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: ≥ 2.5 mg/mL (6.56 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 99.94%

    SDS (393 KB)

    COA (248 KB) LCMS (91 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    To determine the effects of the test compounds (e.g., Opaganib (ABC294640)) on proliferation, cells are plated into 96-well microtiter plates and allowed to attach for 24 h. Varying concentrations of Opaganib are added to individual wells and the cells are incubated for an additional 72 h. At the end of this period, the number of viable cells is determined by use of the sulforhodamine-binding assay. The percentage of cells killed is calculated as the percentage decrease in sulforhodamine-binding compare with control cultures. Regression analyses of inhibition curves are performed by use of GraphPad Prism[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1][3]

    Rats[1]
    Sprague-Dawley male rats (7-8 weeks old) are orally dosed with 0, 100, or 250 mg of ABC294640•HCl/kg in 0.375% Polysorbate-80 in PBS daily for 7 days. The animals are observed daily for viability, signs of gross toxicity, and behavioral changes, and a battery of detailed observations are performed on study days 1 and 7. Blood is sampled from all animals on day 8 of the study for hematology, clinical biochemistry, and serology assessments, and the animals are sacrificed. Gross necropsies are performed on all study rats, and selected organs and tissues are evaluated in the control and high-dose level groups.
    Mice[3]
    Male C57BL/6 (8-9 weeks) mice are gavaged with 50 mg/kg of Opaganib (ABC294640), or an equivalent volume of vehicle (0.375% Tween 80 in phosphate buffered saline, pH 7.1) 1 h before surgery. Under ether anesthesia, ischemia to 70% of the total liver is induced for 1 h. After opening the vascular clamp, the non-ischemic liver lobes are removed, and mice are observed 7 days for survival. Sham operation included equivalent anesthesia and laparotomy without ischemia.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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 2.6253 mL 13.1265 mL 26.2529 mL 65.6323 mL
    5 mM 0.5251 mL 2.6253 mL 5.2506 mL 13.1265 mL
    10 mM 0.2625 mL 1.3126 mL 2.6253 mL 6.5632 mL
    15 mM 0.1750 mL 0.8751 mL 1.7502 mL 4.3755 mL
    20 mM 0.1313 mL 0.6563 mL 1.3126 mL 3.2816 mL
    25 mM 0.1050 mL 0.5251 mL 1.0501 mL 2.6253 mL
    30 mM 0.0875 mL 0.4375 mL 0.8751 mL 2.1877 mL
    40 mM 0.0656 mL 0.3282 mL 0.6563 mL 1.6408 mL
    50 mM 0.0525 mL 0.2625 mL 0.5251 mL 1.3126 mL
    60 mM 0.0438 mL 0.2188 mL 0.4375 mL 1.0939 mL
    80 mM 0.0328 mL 0.1641 mL 0.3282 mL 0.8204 mL
    100 mM 0.0263 mL 0.1313 mL 0.2625 mL 0.6563 mL
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    Opaganib Related Classifications

    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.

    Keywords:

    Opaganib915385-81-8ABC294640ABC 294640ABC-294640SphKSphingosine kinaseInhibitorinhibitorinhibit

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