1. NF-κB
    Immunology/Inflammation
    Apoptosis
  2. Keap1-Nrf2
    STING
    Apoptosis
  3. Omaveloxolone

Omaveloxolone (Synonyms: RTA 408)

Cat. No.: HY-12212 Purity: 99.40%
Handling Instructions

Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.

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

Omaveloxolone Chemical Structure

Omaveloxolone Chemical Structure

CAS No. : 1474034-05-3

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10 mM * 1  mL in DMSO USD 134 In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Omaveloxolone purchased from MCE. Usage Cited in: Oxid Med Cell Longev. 2017;2017:7612182.

    Nuclear translocation of Nrf2 by RTA-408 is measured by immunohistochemistry staining.

    Omaveloxolone purchased from MCE. Usage Cited in: Redox Biol. 2019 Aug 27;28:101309.

    F-Actin ring formation assays are carried to detect the effect of RTA-408 on the generation of mature osteoclasts. The actin rings were detected using phalloidin with fluorescence microscopy after RTA-408 treatment (20 nM).

    Omaveloxolone purchased from MCE. Usage Cited in: Redox Biol. 2019 Aug 27;28:101309.

    The protein level of STING was analyzed by western blotting on day 2 and 4 of osteoclastogenesis in the presence of RTA-408.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.

    IC50 & Target

    Nrf2[1]

    In Vitro

    To evaluate the anti-inflammatory activity of Omaveloxolone (RTA 408), RAW 264.7 mouse macrophage cells are treated with Omaveloxolone for two hours and then IFNγ is added to stimulate NO production and release into the media. Omaveloxolone dose-dependently reduces NO concentrations in the media with an IC50 value of 4.4±1.8 nM. The potency of Omaveloxolone in this assay is similar to that of Bardoxolone methyl, which has an IC50 value of 1.9±0.8 nM. Nrf2 activation is required for AIM-mediated NO suppression. A decrease in nitric oxide synthase 2 (Nos2) protein levels is observed in bardoxolone methyl-treated RAW 264.7 cells, which is attenuated when Nrf2 mRNA levels are reduced by siRNA. To evaluate the anticancer activity of Omaveloxolone, a panel of eight human cell lines derived from tumors of different origin are treated with Omaveloxolone and measured cell growth 72 hours later using the sulforhodamine B (SRB) assay. Omaveloxolone inhibits the growth of all tumor lines with an average GI50 value of 260±74 nM. To determine whether Omaveloxolone induces apoptosis, the panel of tumor cells are treated with Omaveloxolone and the caspase substrate, DEVD-AFC, for 24 hours. Omaveloxolone dose-dependently increases DEVD-AFC cleavage, indicating that Omaveloxolone treatment triggers caspase activation in cancer cells. Caspase-3 and caspase-9 cleavage is also observed by western blot at the same concentrations of Omaveloxolone that increases DEVD-AFC cleavage[1].

    In Vivo

    To determine whether Omaveloxolone (RTA-408) is an effective mitigator of hematopoietic acute radiation syndrome after bone marrow-lethal doses of total-body irradiation (TBI), mice are administered 3 daily injections of 17.5 mg/kg Omaveloxolone beginning 24 h after TBI. Teatment with Omaveloxolone results in the 35 day survival of 100% of 7 Gy (LD40/35) TBI mice (P<0.05) and 60% of 7.5 Gy (LD100/13) TBI mice (P<0.0001)[2].

    Clinical Trial
    Molecular Weight

    554.71

    Formula

    C₃₃H₄₄F₂N₂O₃

    CAS No.

    1474034-05-3

    SMILES

    O=C1C(C#N)=C[[email protected]@]2(C)[[email protected]](CC[[email protected]]([[email protected]@]3(C)[[email protected]@]4([H])[[email protected]@]5([H])[[email protected]@](CCC(C)(C)C5)(NC(C(F)(F)C)=O)CC3)(C)C2=CC4=O)([H])C1(C)C

    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 (180.27 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.8027 mL 9.0137 mL 18.0274 mL
    5 mM 0.3605 mL 1.8027 mL 3.6055 mL
    10 mM 0.1803 mL 0.9014 mL 1.8027 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 2.5 mg/mL (4.51 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [1]

    MEFs, PANC-1, A549, A375, A549/NF-κB-Luc and HeLa/NF-κB-Luc cells are cultured in Gibco high glucose DMEM with 10% FBS. G-361 cells are cultured in McCoy’s 5A medium with 10% FBS. All other cell lines are cultured in RPMI 1640 medium with 10% FBS. For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3×103 cells per well. The following day, one plate is treated with Omaveloxolone (200, 400, 600, 800 and 1000 nM) and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the Omaveloxolone-treated plate are processed for the SRB assay 72 hours after the start of treatment. Percentage of growth relative to vehicle-treated cells is calculated. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated. For cell counting experiments, MEFs are plated in 6-well culture dishes at 5×104 cells per well and treated with Omaveloxolone the following day. Following treatment, cells are counted using a Vi-CELL XR cell analyzer. For clonogenic assays, wild-type (1×103 cells per well) and Keap1-/- (0.5×103 cells per well) MEFs are seeded in 6-well dishes. Six hours later, MEFs are treated with Omaveloxolone. After seven days, colonies are fixed with a 1:7 solution of acetic acid:MeOH and stained with 0.5% crystal violet in MeOH. Colonies consisting of ≥50 cells are counted[1].

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

    Animal Administration
    [2]

    Mice[2]
    For radiation survival experiments, wild-type C57Bl/6 CD45.2 mice (6-8 weeks old) are used. Congenic wild-type C57Bl/6 CD45.1 and C57Bl/6 CD45.1/CD45.2 hybrid host mice are used as recipients in transplantation experiments. Omaveloxolone stock solutions for vehicle control (DMSO) are prepared within 1 h before injection. Omaveloxolone (17.5 mg/kg) or DMSO is administered intraperitoneally at 24, 48 and 72 h after irradiation. Whole-body irradiation (7-8 Gy) is performed using a 250-kVp X-ray machine with 50 cm source-to-skin distance and a 2 mm copper filter. The dose rate is approximately 1.4 Gy/min.

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

    References

    Purity: 99.40%

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    Keywords:

    OmaveloxoloneRTA 408RTA408RTA-408Keap1-Nrf2STINGApoptosisStimulator of Interferon GenesTMEM173MITAERISMPYSInhibitorinhibitorinhibit

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