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532336 NOX Inhibitor VIII, VAS3947 - CAS 869853-70-3 - Calbiochem

532336
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
869853-70-3C₁₄H₁₀N₆OS

Products

Catalogue NumberPackaging Qty/Pack
5323360001 Glass bottle 10 mg
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
CAS number869853-70-3
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
Global Trade Item Number
Catalogue Number GTIN
5323360001 04055977260069

Documentation

NOX Inhibitor VIII, VAS3947 - CAS 869853-70-3 - 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
New Products - Antibodies, Small Molecule, Inhibitors
Pathways and Biomarkers of Oxidative Stress

Technical Info

Title
White Paper: Further considerations of antibody validation and usage.
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
CAS number869853-70-3
Chemical formulaC₁₄H₁₀N₆OS
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage Protect from light
+2°C to +8°C
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.