532336 NOX Inhibitor VIII, VAS3947 - Calbiochem

532336
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₄H₁₀N₆OS

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable triazolo-pyrimidine derivative of VAS2870 (Cat. No. 492000) that displays enhanced solubility and acts as a selective inhibitor NOX family of NADPH oxidase. Shown to inhibit NOX activity in CaCo-2 cells (expressing NOX 1, 2, 4, and 5; IC50 = 12 µM), HL-60 cells (mainly expressing NOX2; IC50 = 2 µM), and A7r5 cells (mainly expressing NOX3 and 4; IC50 = 13 µM). Does not affect the activities of xanthine oxidase and endothelial nitric oxide synthase (eNOS) even at higher concentrations (~100 µM). Acts synergistically with Imatinib (Cat. No. 504595) to reduce the proliferation of chronic myeloid leukemia (CML) cells.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532336
      Brand Family Calbiochem®
      Synonyms3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine, 2-((3-Benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)thio)oxazole, NADPH Oxidase Inhibitor VIII, VAS-3947
      References
      ReferencesSanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
      Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
      Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.
      Product Information
      FormLight yellow solid
      Hill FormulaC₁₄H₁₀N₆OS
      Chemical formulaC₁₄H₁₀N₆OS
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetNADPH Oxidase
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      NOX Inhibitor VIII, VAS3947 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Sanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
      Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
      Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.

      Brochure

      Title
      NPI Flyer- Epigenetics and Nuclear Function Feature (EMD)
      New Products - Antibodies, Small Molecule, Inhibitors
      Pathways and Biomarkers of Oxidative Stress (EMD)

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage. (EMD)
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision05-December-2014 JSW
      Synonyms3-Benzyl-7-(1,3-oxazol-2-ylsulfanyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidine, 2-((3-Benzyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-yl)thio)oxazole, NADPH Oxidase Inhibitor VIII, VAS-3947
      DescriptionA cell-permeable VAS2870 (Cat No. 492000) analogue that displays improved solubility and effectively blocks ROS production in DMSO-differentiated HL-60 cultures upon oxidative burst induction by PMA (IC50 = 1 µM by Cytochrome C reduction & 2 µM by L012 chemiluminescence; Drug added 30 min prior to 100 nM PMA/500582 & 524400) via NADPH oxidases/NOX inhibition, while displaying no potency against eNOS or xanthine oxidase/XOD enzymatic activity in cell-free assays even at a high concentration of 100 µM. Reported to suppress the high ROS level in isolated thoracis aortas sections from spontaneously hypertensive rats (SHRs) in situ (by 66% with 10 µM) and synergize with Imatinib (Cat. No. 504595) against the proliferation of p210 Bcr-abl-expressing murine Boff 210 cultures. A commonly employed NOX inhibitor Apocynin (Cat. No. 178385), in comparison, is shown to interfere with L012-based assays and exhibit little potency against NOX-mediated ROS production in DMSO-differentiated HL-60 cultures (by Cytochrome C reduction) or in cell-free assays using A7r5 & CaCo-2 homogenates (IC50 >1 mM), while another NOX inhibitor DPI (Cat. No. 300260) is shown to inhibit both eNOS & XOD activities.
      FormLight yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₄H₁₀N₆OS
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesSanchez-Sanchez, B., et al. 2014. Clin. Cancer Res. 20, 4014.
      Altenhofer, S., et al., 2012. Cell. Mol. Life Sci. 69, 2327.
      Wind, S., et al. 2010. Br. J. Pharmacol. 161, 885.