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Oltipraz

Catalog No. T0153 CAS 64224-21-1

Synonyms: NSC 347901, RP 35972

Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.

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Oltipraz, CAS 64224-21-1

Pack Size	Availability	Price/USD
5 mg	In stock	$ 31.00
10 mg	In stock	$ 50.00
25 mg	In stock	$ 71.00
50 mg	In stock	$ 89.00
100 mg	In stock	$ 126.00
200 mg	In stock	$ 161.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 99.56%

Purity: 95.91%

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Description	Oltipraz (RP 35972) is a synthetic dithiolethione with potential chemopreventive and anti-angiogenic properties. Oltipraz induces phase II detoxification enzymes, such as glutathione S transferase (GST) and NAD(P)H: quinone oxidoreductase 1 (NQO1). The induction of detoxification enzymes enhances the detoxification of certain cancer-causing agents, thereby enhancing their elimination and preventing carcinogen-induced DNA damages. Although the exact mechanism through which the anti-angiogenesis effect remains to be fully elucidated, oltipraz maybe able to modulate the expression of a number of angiogenic factors, thereby blocking the sustained and focal neovascularization in multiple tumor cell types.
Targets&IC50	HIF1α:10 μM
In vitro	Oltipraz, as a chemoprotective agent, induces Phase II detoxification enzyme activity in a Nrf2-dependent manner. [1] 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. [2]
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. [1] 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. [2] In rats on a CDAA diet, Oltipraz attenuate the progression of nonalcoholic steatohepatitis-related fibrosis. [3]
Kinase Assay	The Src and Abl kinase assays: The Src kinase activity is measured in an ELISA format. Src (3 units/reaction), reaction buffer (50 mM Tris-HCl pH 7.5, 10 mM MgCl2, 0.1 mM EGTA, 0.5 mM Na3VO4) and cdc2 substrate peptide are added to various concentration of Bosutinib and incubated at 30 °C for 10 minutes. The reaction is started by the addition of ATP to a final concentration of 100 μM, incubated at 30 °C for 1 hour and stopped by addition of EDTA. Instructions from the manufacturer are followed for subsequent steps. The Abl kinase assay is performed in a DELFIA solid phase europium-based detection assay format. Biotinylated peptide (2 μM) is bound to streptavidin-coated microtitration plates for 1.5 hours in 1 mg/mL ovalbumin in PBS. The plates are washed for 1 hour with PBS/0.1% Tween 80, followed by a PBS wash. The kinase reaction is incubated for 1 hour at 30°C. Abl kinase (10 units) is mixed with 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, 80 μM EGTA, 100 μM ATP, 0.5 mM Na3VO4, 1% DMSO, 1 mM HEPES (pH 7.0), 200 μg/mL ovalbumin and various concentration of Bosutinib. The reaction is stopped with EDTA at a final concentration of 50 mM. The reaction is monitored with Eu-labeled phosphotyrosine antibody and DELFIA enhancement solution.

Synonyms	NSC 347901, RP 35972
Molecular Weight	226.34
Formula	C8H6N2S3
CAS No.	64224-21-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11.3 mg/mL (50 mM)

References and Literature

1. Ramos-Gomez M, et al. Proc Natl Acad Sci U S A. 2001, 98(6), 3410-3415.. 2. Lee WH, et al. Mol Cancer Ther. 2009, 8(10), 2791-2802. 3. Shimozono R, et al. Mol Pharmacol. 2013, 84(1), 62-70.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Metabolism Compound Library Anti-Lung Cancer Compound Library Anti-Infection Compound Library HIF-1 Signaling Pathway Compound Library Anti-Pancreatic Cancer Compound Library

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Keywords

Oltipraz 64224-21-1 Angiogenesis Chromatin/Epigenetic Immunology/Inflammation Metabolism Microbiology/Virology Proteases/Proteasome Reverse Transcriptase Nrf2 HIF/HIF Prolyl-Hydroxylase HIV Protease HIF Inhibitor Keap1-Nrf2 RP35972 inhibit HIFs Human immunodeficiency virus HIV Hypoxia-inducible factors NSC347901 NSC-347901 RP-35972 NSC 347901 RP 35972 HIF-PH inhibitor

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