RRx-001

Catalog No.S8405

For research use only.

RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.

RRx-001 Chemical Structure

CAS No. 925206-65-1

Selleck's RRx-001 has been cited by 3 Publications

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Biological Activity

Description RRx-001 is a novel epigenetic modulator with potential radiosensitizing activity. It inhibits glucose 6-phosphate dehydrogenase(G6PD) in human tumor cells, binds hemoglobin and drives RBC-mediated redox reactions under hypoxia. RRx-001 triggers apoptosis and exhibits anticancer activity.
Targets
G6PD [1] Nrf2-ARE [3]
In vitro

RRx-001 exerts its anti-proliferative effect, at least partially, through interference with glucose 6 phosphate dehydrogenase (G6PD), a key enzyme in the pentose phosphate pathway, responsible for maintaining adequate levels of the major cellular reductant, NADPH. RRx-001 affects glucose and G6PD enzyme activity in three different cancer cell lines namely Hep G2, CACO-2, and HT-29. RRx-001 induced G6PD inhibition and increased glucose consumption in a concentration dependent fashion. RRx-001 induces p53 and PARP-1 via generation of ROS/RNS. It exerts anticancer activity, at least in part, by interfering with 3 crucial metabolic demands of rapidly proliferating cells: bioenergetics, macromolecular biosynthesis, and manipulation of cellular cytosolic redox homeostasis[1]. RRx-001 mediates nuclear translocation of Nrf2 and the activation of expression of its downstream enzymes HO-1 and NQO1 in tumor cells. Apart from epigenetic alterations, RRx-001 acts via pleiotropic mechanisms including redox signaling and redox-induced dysregulation of many different signal pathways such as Nrf2, p53, PARP cleavage, HIF1 alpha, and G6PD activity. It also triggers p53 and p21 activity in response to double-stranded DNA breaks as well as deregulates cancer cellular energetics and metabolism. RRx-001 is a potent activator of the Nrf2-ARE signaling pathway via ROS/RNS generation[3].

In vivo RRx-001 shows promise for short-term blood flow redistribution in tumors with a pericyte- and α-SMA-rich vasculature[2]. RRx-001 monotherapy is well tolerated, with no dose-limiting toxicities. It not only facilitates nuclear translocation of Nrf2, but also upregulates endogenous Nrf2 expression in SCC VII tumors in mice[3].

Protocol (from reference)

Cell Research:[1]
  • Cell lines: Human cell cancer lines HEP-G2, HT-29 and CACO-2
  • Concentrations: 5, 50, and 100 μM
  • Incubation Time: up to 72 h
  • Method: Cell growth and proliferation is assessed using the MTT proliferation assay kit. Briefly, 5×103 cells are seeded in each well of a 96-well plate and cells are treated with or without compounds. Cells are cultured for up to 72 h. MTT reagent (10 μL) is added to each well, and then incubate for 3 h. Post incubation, the culture medium is removed, 100 μL Crystal Dissolving Solution is added to each well, and the absorbance of the solution is measured at 570 nm. MTT assays for samples of the same conditions are performed in triplicate. Briefly, MTT solution (0.5 mg/mL) is added, cells are incubated at 37ºC for 4 h and absorption at 540 nm is measured using a microplate reader.
Animal Research:[2]
  • Animal Models: C3H mice/SCID mice
  • Dosages: 15 mg/kg
  • Administration: i.v.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 268.02
Formula

C5H6BrN3O5

CAS No. 925206-65-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1C(CN1C(=O)CBr)([N+](=O)[O-])[N+](=O)[O-]

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02452970 Terminated Drug: RRx-001|Drug: Gemcitabine and cisplatin Cholangiocarcinoma EpicentRx Inc. July 16 2015 Phase 2
NCT02096341 Terminated Drug: RRx-001 Malignant Solid Tumor|Lymphomas EpicentRx Inc. April 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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