1. Immunology/Inflammation
  2. SPHK
  3. Opaganib

Opaganib (Synonyms: ABC294640)

Cat. No.: HY-16015 Purity: 99.68%
Handling Instructions

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 Stock
10 mM * 1 mL in DMSO Get quote
5 mg USD 96 Get quote
10 mg USD 168 Get quote
50 mg USD 528 Get quote
100 mg USD 888 Get quote

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Top Publications Citing Use of Products

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

    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.

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

    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 MCE. Usage Cited in: Arch Med Res. 2018 Jul;49(5):335-341.

    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.
    • Biological Activity

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    • References

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    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].

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

    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].

    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.

    915385-81-8

    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)

    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
    10 mM 0.2625 mL 1.3126 mL 2.6253 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 (6.56 mM); Clear solution

    • 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

    • 3.

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

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

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.68%

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    Keywords:

    OpaganibABC294640ABC 294640ABC-294640SPHKSphingosine kinaseInhibitorinhibitorinhibit

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    Cat. No.:
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