Home NF-κB NF-κB inhibitor - Nrf2 activator Omaveloxolone (RTA-408) For research use only.

Omaveloxolone (RTA-408)

Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.

Omaveloxolone (RTA-408) Chemical Structure

Omaveloxolone (RTA-408) Chemical Structure

CAS No. 1474034-05-3

Purity & Quality Control

Omaveloxolone (RTA-408) Related Products

Signaling Pathway

NF-κB Signaling Pathways

NF-κB Signaling Pathway

Biological Activity

Description Omaveloxolone (RTA-408) is a synthetic triterpenoid that activates the cytoprotective transcription factor Nrf2 and inhibits NF-κB signaling. Phase 2.
Targets
NF-κB [1] Nrf2 [1]
In vitro
In vitro RTA 408 potently increases expression of Nrf2 target genes and reverses IFNγ-mediated suppression of Gclc expression in RAW 264.7 cells. In a panel of eight human tumor cell lines, RTA 408 inhibits growth with an average GI50 value of 260 nM and induces apoptosis. RTA 408 also inhibits NF-κB and activates JNK in tumor cells. [1]
Cell Research Cell lines A375, NCI-H460, A2058, MDA-Mb-231, HCT116, 786-0, A549, and PANC-1 cells
Concentrations ~1 μM
Incubation Time 72 hours
Method For growth inhibition assays, cells are plated in duplicate 96-well culture dishes at 3 x 103 cells per well. The following day, one plate is treated with RTA 408 and the other is immediately processed for the sulforhodamine B (SRB) assay (time 0). Cells in the RTA 408-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 using: [(Ti-Tz)/(C-Tz)] x 100 where (Tz) is the absorbance value at time zero, (C) is absorbance value from vehicle treated wells after 72 hours, and (Ti) is the absorbance value from wells treated with the drug. Dose-response curves are plotted in GraphPad Prism and GI50 values are calculated
In Vivo
In vivo In mice with radiation-induced dermatitis, 1.0% RTA 408 markedly reduces epidermal and collagen thickening, prevents dermal necrosis and completely alleviates skin ulcers. [2] In rat skin, RTA 408 activates Nrf2 and induces cytoprotective genes. [3] RTA 408 also mitigates hematopoietic acute radiation syndrome in mice. [4]
Animal Research Animal Models Mice with radiation-induced dermatitis
Dosages 1% in 100 μL vehicle (w/v)
Administration Topical application
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06054893 Not yet recruiting
Friedreich Ataxia
Biogen
 November 1 2023 Phase 1
NCT05909644 Completed
Healthy Adult Subjects
Reata a wholly owned subsidiary of Biogen|Celerion|Q2 Solutions|Altasciences Company Inc.|Biogen
 July 5 2023 Phase 1
NCT03902002 Completed
Hepatic Impairment
Reata a wholly owned subsidiary of Biogen|Biogen
 July 19 2019 Phase 1
NCT03931590 Completed
Healthy Male Subjects
Reata a wholly owned subsidiary of Biogen|Biogen
 April 11 2019 Phase 1
NCT03664453 Completed
Healthy
Reata a wholly owned subsidiary of Biogen|Biogen
 October 29 2018 Phase 1

Chemical Information & Solubility

Molecular Weight 554.71 Formula

C33H44F2N2O3
CAS No. 1474034-05-3 SDF Download Omaveloxolone (RTA-408) SDF
Smiles CC1(CCC2(CCC3(C(C2C1)C(=O)C=C4C3(CCC5C4(C=C(C(=O)C5(C)C)C#N)C)C)C)NC(=O)C(C)(F)F)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (180.27 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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