Cat. No.: HY-16438

RRx-001

(Synonyms: Nibrozetone)

20 Cited Publications

Customer Review

Based on 20 publication(s) in Google Scholar

RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity.

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

Purity: 99.79%
CAS No.: 925206-65-1
Formula: C₅H₆BrN₃O₅
Molecular Weight:268.02

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

RRx-001 Chemical Structure

CAS No.: 925206-65-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (20)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

RRx-001, a hypoxia-selective epigenetic agent and studied as a radio- and chem-sensitizer, triggers apoptosis and overcomes agent resistance in myeloma. RRx-001 exhibits potent anti-tumor activity with minimal toxicity^[1]. RRx-001 is a dual small molecule checkpoint inhibitor by downregulating CD47 and SIRP-α^[2]. RRx-001 is a potent inhibitor of G6PD and shows potent antimalarial activity^[3].

IC₅₀ & Target

Plasmodium

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A498	IC₅₀	4.9 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human A498 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
A549	IC₅₀	6 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
HT-29	IC₅₀	3.4 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
IMR-32	IC₅₀	5.1 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human IMR-32 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
M21	IC₅₀	2.6 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human M21 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
MCF7	IC₅₀	4 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
PANC-1	IC₅₀	2.3 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
RKO	IC₅₀	3 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human RKO cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
SCC-7	IC₅₀	1.8 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against mouse SCC-7 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
SNB-75	IC₅₀	3.8 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human SNB-75 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
U-87MG ATCC	IC₅₀	2.7 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human U87 cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]
UMSCC22B	IC₅₀	2.3 pM Compound: RRx-001; ABDNAZ	Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay Antiproliferative activity against human UMSCC22B cells assessed as cell growth inhibition by CCK8 assay	[PMID: 34043360]

In Vitro

RRx-001 (0-5 μM, 24 hours) inhibits MM cells growth and overcomes resistance to novel and conventional therapies^[1].
RRx-001 blocks migration of MM cells and associated angiogenesis^[1].
RRx-001 induces significant G1 phase growth arrest, with a concomitant decrease in the S phase. RRx-001 triggers significant apoptosis in MM cells^[1].
RRx-001 inhibits DNA methylation by downregulating DNA methytransferases^[1].
RRx-001 and the supernatant of RRx-001-treated macrophages downregulates CD47 on tumor cells and SIRPα on macrophages^[2].

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

Cell Viability Assay^[1]

Cell Line:

Human MM-cell lines (MM.1S, RPMI-8226, H929, ARP1, KMS-11, OPM2, LR5, ANBL6.WT), along with drug resistant cell lines such as (MM.1R, Dox40, LR5, ANBL6.BR, RPMI-8226).
Concentration:

0-5 μM.
Incubation Time:

24 hours.
Result:

Induced a dose-dependent significant (p < 0.05) decrease in viability of all cell lines.

In Vivo

RRx-001 (5 mg/kg or 10 mg/kg, I.V., thrice-weekly for 24 days) inhibits tumor growth and prolongs survival in a xenograft mouse model^[1].
RRx-001 (10 mg/kg, IP, twice a week and once a day) exhibits potent anti-cancer activity on the A549 lung cancer model dependent on the presence of tumor-associated macrophages (TAMs) in tumor tissue^[2].

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

Animal Model:

CB-17 SCID-mice were subcutaneously inoculated with 5.0 × 10⁶ MM.1S cells in 100 µL of serum-free RPMI 1640 medium^[1].
Dosage:

5 mg/kg or 10 mg/kg.
Administration:

I.V., thrice-weekly for 24 days.
Result:

Blocked MM tumor growth and enhances survival.
Treatment was well tolerated, suggested by no apparent weight loss.

Animal Model:

Female BALB/c nude mice (19.2 ± 1.7 g) based on A549 lung cancer model^[2].
Dosage:

10 mg/kg.
Administration:

IP, twice a week and once a day.
Result:

Resulted in the most significant tumor growth retardation.
Reduction of resident macrophages in tumor-bearing mice attenuates the antitumor activity of RRx-001.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 925206-65-1
Appearance Solid
Molecular Weight 268.02
Formula C₅H₆BrN₃O₅
Color White to off-white
SMILES

BrCC(N1CC([N+]([O-])=O)([N+]([O-])=O)C1)=O
Synonyms

Nibrozetone
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

Publications (20)

All WB

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Journal Impact Factor

Nat Biomed Eng

A live bacteria enzyme assay for identification of human disease mutations and drug screening. [Abstract]

2025 Sep;9(9):1547-1556. PMID: 40307426
Nat Commun

Microglia alter sex-specific cerebellar myelination following placental hormone loss. [Abstract]

2025 Nov 7;16(1):9846. PMID: 41203610
Nat Commun

Clustering of NLRP3 induced by membrane or protein scaffolds promotes inflammasome assembly. [Abstract]

2025 May 27;16(1):4887. PMID: 40425567
Nat Commun

Nanomedicine-based co-delivery of a calcium channel inhibitor and a small molecule targeting CD47 for lung cancer immunotherapy. [Abstract]

2023 Nov 11;14(1):7306. PMID: 37951973
Mol Cell

One-Carbon Metabolism Supports S-Adenosylmethionine and Histone Methylation to Drive Inflammatory Macrophages. [Abstract]

2019 Sep 19;75(6):1147-1160.e5. PMID: 31420217
J Exp Clin Cancer Res

CCDC6 and USP7 expression levels suggest novel treatment options in high-grade urothelial bladder cancer. [Abstract]

2019 Feb 20;38(1):90. PMID: 30786932

RRx-001 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90. [Abstract]

Protein levels of DNMT1 and CCDC6 in J82 cells treated with different concentrations of RRx-001, as determined by western blot. Vinculin and Tubulin are used as internal controls for sample loading. 5-AZA is used as positive control for inhibition of DNMT1 expression.

RRx-001 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2019 Feb 20;38(1):90. [Abstract]

Whole cell lysates from J82 shCCDC6 or shCTRL cells, treated with different concentrations of RRx-001, or untreated, are immunoblotted with anti-CCDC6 antibody. γH2AX levels are shown. Tubulin is used as loading control.
Cell Rep Med

KRASG12D-driven pentose phosphate pathway remodeling imparts a targetable vulnerability synergizing with MRTX1133 for durable remissions in PDAC. [Abstract]

2025 Feb 18;6(2):101966. PMID: 39970873
Biomaterials

CD40 agonist engineered immunosomes modulated tumor microenvironment and showed pro-immunogenic response, reduced toxicity, and tumor free survival in mice bearing glioblastoma. [Abstract]

2024 Dec:311:122688. PMID: 38943821
Acta Biomater

Promotion of triple negative breast cancer immunotherapy by combining bioactive radicals with immune checkpoint blockade. [Abstract]

2025 Mar 1:194:305-322. PMID: 39805523
Proc Natl Acad Sci U S A

NSUN5/TET2-directed chromatin-associated RNA modification of 5-methylcytosine to 5-hydroxymethylcytosine governs glioma immune evasion. [Abstract]

2024 Apr 2;121(14):e2321611121. PMID: 38547058
Antioxidants (Basel)

Investigation of a UPR-Related Gene Signature Identifies the Pro-Fibrotic Effects of Thrombospondin-1 by Activating CD47/ROS/Endoplasmic Reticulum Stress Pathway in Lung Fibroblasts. [Abstract]

2023 Nov 21;12(12):2024. PMID: 38136144
J Med Chem

Enhanced Immunotherapy Based on Combining the Pro-phagocytosis and Anti-phagocytosis Checkpoint Blockade for Tumor Eradication. [Abstract]

2022 Nov 10;65(21):14832-14842. PMID: 36260348
J Virol

Newcastle Disease Virus Manipulates Mitochondrial MTHFD2-Mediated Nucleotide Metabolism for Virus Replication. [Abstract]

2023 Mar 30;97(3):e0001623. PMID: 36794935

RRx-001 purchased from MedChemExpress. Usage Cited in: J Virol. 2023 Mar 30;97(3):e0001623. [Abstract]

RRx-001 (2.5, 5, 10, 20, 100 µM; 12 h) significantly and dose-dependently reduces Newcastle disease virus (NDV) NP protein expression in NDV-infected cells.
J Mol Neurosci

Therapeutic Hypothermia and Recombinant Erythropoietin Mitigate Brain Microvascular Endothelial Cell Dysfunction via Modulating the Pentose Phosphate Pathway. [Abstract]

2025 May 9;75(2):65. PMID: 40343581
Patent

US20240325538A1.
Columbia University

2024 Jun 26.
Patent

US20240238271A1.
Patent

US20230226111A1.
bioRxiv

Covalent targeting as a common mechanism for inhibiting NLRP3 inflammasome assembly. [Abstract]

2023 Jun 1:2023.06.01.543248. PMID: 37398499
Biomed Pharmacother

Inhibition of Nrf2-mediated glucose metabolism by brusatol synergistically sensitizes acute myeloid leukemia to Ara-C. [Abstract]

2021 Oct:142:111652. PMID: 34112534

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (373.11 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.7311 mL

18.6553 mL

37.3107 mL

5 mM

0.7462 mL

3.7311 mL

7.4621 mL

10 mM

0.3731 mL

1.8655 mL

3.7311 mL

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

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (9.33 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (9.33 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (9.33 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (644 KB)
- English - EN (644 KB)
- Français - FR (644 KB)
- Deutsch - DE (644 KB)
- Norwegian - NO (644 KB)
- Español - ES (644 KB)
- Swedish - SV (644 KB)
- Italian - IT (644 KB)
- Korean - KR (644 KB)
- Portuguese - PT (644 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Das DS, et al. A novel hypoxia-selective epigenetic agent RRx-001 triggers apoptosis and overcomes drug resistance in multiple myeloma cells. Leukemia. 2016 Nov;30(11):2187-2197. [Content Brief]

[2]. Yalcin O, et al. From METS to malaria: RRx-001, a multi-faceted anticancer agent with activity in cerebral malaria. Malar J. 2015 May 28;14:218. [Content Brief]

[3]. Cabrales P, et al. RRx-001 Acts as a Dual Small Molecule Checkpoint Inhibitor by Downregulating CD47 on Cancer Cells and SIRP-α on Monocytes/Macrophages. Transl Oncol. 2019 Apr;12(4):626-632. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	3.7311 mL	18.6553 mL	37.3106 mL	93.2766 mL
	5 mM	0.7462 mL	3.7311 mL	7.4621 mL	18.6553 mL
	10 mM	0.3731 mL	1.8655 mL	3.7311 mL	9.3277 mL
	15 mM	0.2487 mL	1.2437 mL	2.4874 mL	6.2184 mL
	20 mM	0.1866 mL	0.9328 mL	1.8655 mL	4.6638 mL
	25 mM	0.1492 mL	0.7462 mL	1.4924 mL	3.7311 mL
	30 mM	0.1244 mL	0.6218 mL	1.2437 mL	3.1092 mL
	40 mM	0.0933 mL	0.4664 mL	0.9328 mL	2.3319 mL
	50 mM	0.0746 mL	0.3731 mL	0.7462 mL	1.8655 mL
	60 mM	0.0622 mL	0.3109 mL	0.6218 mL	1.5546 mL
	80 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1660 mL
	100 mM	0.0373 mL	0.1866 mL	0.3731 mL	0.9328 mL

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RRx-001

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Rare Diseases Drug Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RRx-001

All Parasite Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RRx-001

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Rare Diseases Drug Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) RRx-001

All Parasite Isoforms

Biological Activity

Chemical Information

Publications (20)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

RRx-001 Related Classifications

HY-16438 Related Classifications