Oltipraz
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 : 99.87%
- CAS No.: 64224-21-1
- Formula: C8H6N2S3
- Molecular Weight:226.34
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Oltipraz
More- Redox Biol. 2024 Aug:74:103225. [Abstract]
- J Nanobiotechnology. 2025 Jan 29;23(1):60. [Abstract]
- Cell Death Dis. 2025 Apr 1;16(1):232. [Abstract]
- Acta Pharmacol Sin. 2020 Aug;41(8):1041-1048. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Free Radic Biol Med. 2025 Apr 25:S0891-5849(25)00250-3. [Abstract]
- Aging Cell. 2021 Oct;20(10):e13483. [Abstract]
- Cell Prolif. 2021 Dec;54(12):e13142. [Abstract]
- Integrative Medicine in Nephrology and Andrology. 2025 Mar.
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Ethnopharmacol. 2021 Nov 15:280:114411. [Abstract]
- Eur J Pharmacol. 2022 Dec 5:936:175361. [Abstract]
- J Endocrinol. 2021 May;249(2):83-93. [Abstract]
- J Endocrinol. 2017 Aug;234(2):73-87. [Abstract]
- Int Immunopharmacol. 2025 Dec 10:167:115655. [Abstract]
- Int Immunopharmacol. 2025 Oct 30:164:115309. [Abstract]
- Int Immunopharmacol. 2020 Jul:84:106570. [Abstract]
- J Biol Chem. 2022 Dec;298(12):102678. [Abstract]
- Curr Med Sci. 2023 Aug;43(4):689-695. [Abstract]
- Scienceasia. 2024 Apr 13.
- Int J Biol Macromol. 2023 Dec 31;253(Pt 8):127575. [Abstract]
- Research Square Preprint. 2023 Oct 23.
All Parasite Isoforms
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Biological Activity
Description
IC50 & Target
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. Further protocols information, click here.
In Vivo
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 64224-21-1
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Appearance Solid
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Molecular Weight 226.34
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Formula C8H6N2S3
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Color Brown to red
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SMILES
S=C1SSC(C2=NC=CN=C2)=C1C
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Synonyms
RP 35972; NSC 347901
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Shipping
Room temperature in continental US; may vary elsewhere.
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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
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Most Recent
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Redox Biol
FAM3A plays a key role in protecting against tubular cell pyroptosis and acute kidney injury. [Abstract]2024 Aug:74:103225. PMID: 38875957 -
J Nanobiotechnology
CT-sensitized nanoprobe for effective early diagnosis and treatment of pulmonary fibrosis. [Abstract]2025 Jan 29;23(1):60. PMID: 39881299 -
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
2020 Aug;41(8):1041-1048. PMID: 32203087 -
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 -
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 -
Aging Cell
Identification of a small molecule SR9009 that activates NRF2 to counteract cellular senescence. [Abstract]2021 Oct;20(10):e13483. PMID: 34587364 -
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 -
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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 -
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 -
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 -
J Endocrinol
2021 May;249(2):83-93. PMID: 33705351 -
J Endocrinol
2017 Aug;234(2):73-87. PMID: 28515141 -
Int Immunopharmacol
The Nrf2/GPX4 antioxidant pathway suppresses ferroptosis to protect against hearing impairment in cochlear ischemia-reperfusion injury. [Abstract]2025 Dec 10:167:115655. 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 Oct 30:164:115309. PMID: 40811944 -
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 -
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 -
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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 : 12.5 mg/mL (55.23 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
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Data Sheet (281 KB)
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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)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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]
Complete Stock Solution Preparation Table
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.
| 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 | |
| 30 mM | 0.1473 mL | 0.7364 mL | 1.4727 mL | 3.6818 mL | |
| 40 mM | 0.1105 mL | 0.5523 mL | 1.1045 mL | 2.7613 mL | |
| 50 mM | 0.0884 mL | 0.4418 mL | 0.8836 mL | 2.2091 mL |
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