Cat. No.: HY-12519

Oltipraz

(Synonyms: RP 35972; NSC 347901)

22 Cited Publications

Customer Review

Based on 22 publication(s) in Google Scholar

Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC₅₀ of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.

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

Purity: 99.71%
CAS No.: 64224-21-1
Formula: C₈H₆N₂S₃
Molecular Weight:226.34

Storage:

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

Oltipraz Chemical Structure

CAS No.: 64224-21-1

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (22)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 10 μM (HIF-1α)^[1];
Nrf2^[4]

All HIF/HIF Prolyl-Hydroxylase Isoforms :

All HIV Isoforms :

All Parasite Isoforms :

In Vitro

Oltipraz inhibits HIF-1α activity and HIF-1α-dependent tumor growth, which may result from a decrease in HIF-1α stability through S6K1 inhibition in combination with an H2O2-scavenging effect. Oltipraz treatment also inhibits HIF-1α activation stimulated by either hypoxia or CoCl2. Oltipraz is a cancer chemopreventive agent and has an inhibitory effect on angiogenesis and tumor growth. [1] Oltipraz is also a competitive inhibitor of this cytochrome P450, with an apparent Ki of 10 μM. [2]

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

In Vivo

In wild-type mice, hepatic levels of mRNA for all of the genes analyzed were significantly increased after Oltipraz treatment, with the highest increase (treated/control) for NQO1 mRNA levels (7.6-fold). The Northern blot analyses demonstrated that the observed increases in GST and NQO1 activities by Oltipraz in wild-type mice were preceded by significant elevations in RNA expression. Interestingly, mRNA levels of Nrf2 itself were increased more than 3-fold by Oltipraz treatment. [2]

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

Clinical Trial

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

Chemical Information

CAS No. 64224-21-1
Appearance Solid
Molecular Weight 226.34
Formula C₈H₆N₂S₃
Color Brown to red
SMILES

S=C1SSC(C2=NC=CN=C2)=C1C
Synonyms

RP 35972; NSC 347901
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (22)

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Journal Impact Factor

J Nanobiotechnology

CT-sensitized nanoprobe for effective early diagnosis and treatment of pulmonary fibrosis. [Abstract]

2025 Jan 29;23(1):60. PMID: 39881299
Redox Biol

FAM3A plays a key role in protecting against tubular cell pyroptosis and acute kidney injury. [Abstract]

2024 Jun 8:74:103225. PMID: 38875957
Cell Death Dis

SIRT7-mediated NRF2 deacetylation promotes antioxidant response and protects against chemodrug-induced liver injury. [Abstract]

2025 Apr 1;16(1):232. PMID: 40169535
Acta Pharmacol Sin

Nrf2 activation ameliorates mechanical allodynia in paclitaxel-induced neuropathic pain. [Abstract]

2020 Aug;41(8):1041-1048. PMID: 32203087
Free Radic Biol Med

Methionine sulfoxide reductase A deficiency aggravated ferroptosis in LPS-induced acute kidney injury by inhibiting the AMPK/NRF2 axis and activating the CaMKII/HIF-1α pathway. [Abstract]

2025 Apr 25:S0891-5849(25)00250-3. PMID: 40288699
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Aging Cell

Identification of a small molecule SR9009 that activates NRF2 to counteract cellular senescence. [Abstract]

2021 Oct;20(10):e13483. PMID: 34587364
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Cell Prolif

CoCrMo-Nanoparticles induced peri-implant osteolysis by promoting osteoblast ferroptosis via regulating Nrf2-ARE signalling pathway. [Abstract]

2021 Dec;54(12):e13142. PMID: 34632658
J Ethnopharmacol

Yi-Qi-Jian-Pi formula modulates the PI3K/AKT signaling pathway to attenuate acute-on-chronic liver failure by suppressing hypoxic injury and apoptosis in vivo and in vitro. [Abstract]

2021 Nov 15:280:114411. PMID: 34265380
Int Immunopharmacol

The Nrf2/GPX4 antioxidant pathway suppresses ferroptosis to protect against hearing impairment in cochlear ischemia-reperfusion injury. [Abstract]

2025 Oct 15:167:115655. PMID: 41101226
Int Immunopharmacol

Rutin alleviates preoperative anxiety stress-induced persistent postoperative pain by inhibiting microglia-mediated abnormal synaptic engulfment in the spinal cord dorsal horn. [Abstract]

2025 Aug 13:164:115309. PMID: 40811944
Eur J Pharmacol

Oltipraz, the activator of nuclear factor erythroid 2-related factor 2 (Nrf2), protects against the formation of BAPN-induced aneurysms and dissection of the thoracic aorta in mice by inhibiting activation of the ROS-mediated NLRP3 inflammasome. [Abstract]

2022 Dec 5:936:175361. PMID: 36336010
Int Immunopharmacol

Cinnamaldehyde suppresses NLRP3 derived IL-1β via activating succinate/HIF-1 in rheumatoid arthritis rats. [Abstract]

2020 Jul:84:106570. PMID: 32413739
J Biol Chem

Antidiabetic drug metformin suppresses tumorigenesis through inhibition of mevalonate pathway enzyme HMGCS1. [Abstract]

2022 Dec;298(12):102678. PMID: 36356901
J Endocrinol

Novel adipokine asprosin modulates browning and adipogenesis in white adipose tissue. [Abstract]

2021 May;249(2):83-93. PMID: 33705351
J Endocrinol

Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. [Abstract]

2017 Aug;234(2):73-87. PMID: 28515141
Curr Med Sci

Hypoxia Affects Autophagy in Human Umbilical Vein Endothelial Cells via the IRE1 Unfolded Protein Response. [Abstract]

2023 Aug;43(4):689-695. PMID: 37558862
Scienceasia

2024 Apr 13.
Integrative Medicine in Nephrology and Andrology

2025 Mar.
Research Square Preprint

2023 Oct 23.
Int J Biol Macromol

STC2 is a potential biomarker of hepatocellular carcinoma with its expression being upregulated in Nrf1α-deficient cells, but downregulated in Nrf2-deficient cells. [Abstract]

2023 Dec 31;253(Pt 8):127575. PMID: 37866563

Solvent & Solubility

In Vitro:

DMSO : 6 mg/mL (26.51 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

4.4181 mL

22.0907 mL

44.1813 mL

5 mM

0.8836 mL

4.4181 mL

8.8363 mL

10 mM

0.4418 mL

2.2091 mL

4.4181 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator

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

Mass

Concentration

Volume

Molecular Weight

Dilution Calculator

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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 1 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% Corn Oil

Solubility: ≥ 1 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 1 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 (10.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
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 (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Portuguese - PT (396 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]. Lee WH, et al. Oltipraz and dithiolethione congeners inhibit hypoxia-inducible factor-1alpha activity through p70 ribosomal S6 kinase-1 inhibition and H2O2-scavenging effect. Mol Cancer Ther. 2009 Oct;8(10):2791-802. [Content Brief]

[2]. Lv S, et al. Glucagon-induced extracellular cAMP regulates hepatic lipid metabolism. J Endocrinol. 2017 Aug;234(2):73-87. [Content Brief]

[3]. Ramos-Gomez M, et al. Sensitivity to carcinogenesis is increased and chemoprotective efficacy of enzyme inducers is lost in nrf2 transcription factor-deficient mice. Proc Natl Acad Sci U S A. 2001 Mar 13;98(6):3410-5. [Content Brief]

[4]. Eba S, et al.The nuclear factor erythroid 2-related factor 2 activator oltipraz attenuates chronic hypoxia-induced cardiopulmonary alterations in mice.Am J Respir Cell Mol Biol. 2013 Aug;49(2):324-33. [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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.4181 mL	22.0907 mL	44.1813 mL	110.4533 mL
	5 mM	0.8836 mL	4.4181 mL	8.8363 mL	22.0907 mL
	10 mM	0.4418 mL	2.2091 mL	4.4181 mL	11.0453 mL
	15 mM	0.2945 mL	1.4727 mL	2.9454 mL	7.3636 mL
	20 mM	0.2209 mL	1.1045 mL	2.2091 mL	5.5227 mL
	25 mM	0.1767 mL	0.8836 mL	1.7673 mL	4.4181 mL

Keywords

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Oltipraz

Anti-Infection Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Metabolism/Protease Compound Library

NF-κB Signaling Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Antiviral Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Antioxidant Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Ferroptosis Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Transcription Factor-Targeted Library

Targeted Diversity Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Metabolic Enzyme Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Fibrosis Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Oltipraz

All HIF/HIF Prolyl-Hydroxylase Isoforms

All HIV Isoforms

All Parasite Isoforms

Biological Activity

Chemical Information

Publications (22)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Oltipraz Related Classifications

Cat. No.: HY-12519