Molecular Weight(MW): 226.34
Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.
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Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining. Effects of p21 depletion and Nrf2 activation on dexamethasone-induced apoptosis in MC3T3-E1 cells. Cells were transfected with control siRNA or p21 siRNA. Subsequently, transfected cells were pre-incubated with oltipraz (20 μM) for 1 h, and then co-incubated with 1 μM dexamethasone for 24 h. Apoptosis was measured by flow cytometry, followed by Annexin V-FITC/PI double staining.
Arch Toxicol, 2017. Oltipraz purchased from Selleck.
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Choose Selective Nrf2 Inhibitors
|Description||Oltipraz is a potent Nrf2 activator and a potent inducer of Phase II detoxification enzymes, most notably glutathione-S-transferase (GST). Phase 3.|
Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner.  In human HT29 colon cancer cells, oltipraz inhibits the induction of HIF-1α by insulin, hypoxia or CoCl2 by significantly accelerating degradation of HIF-1α protein. 
|In vivo||Oltipraz (500 mg/kg, p.o.) significantly reduces multiplicity of gastric neoplasia in wild-type mice by 55%, but has no effect on tumor burden in nrf2-deficient mice.  In BALB/c nude mice transplanted with HCT116 cells, Oltipraz (200 mg/kg, p.o.) inhibits tumor growth and angiogenesis via inhibition of HIF-1α.  In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis. |
|In vitro||DMSO||39 mg/mL warmed (172.3 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02068339||Completed||Non-alcholic Fatty Liver Disease||PharmaKing||February 2014||Phase 3|
|NCT01373554||Completed||Non-alcoholic Fatty Liver Disease||PharmaKing||May 2011||Phase 2|
|NCT00956098||Completed||Liver Fibrosis|Liver Cirrhosis||CJ HealthCare Corporation||February 2006||Phase 2|
|NCT00006457||Completed||Lung Cancer||Northwestern University|National Cancer Institute (NCI)||August 2000||Phase 1|
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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