533718 NOD2 Signaling Inhibitor II, GSK717

533718
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      Overview

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      5.33718.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable benzimidazole diamide compound that acts as a potent, selective, reversible and muramyl dipeptide (MDP)-induced NOD2 (MDP/nucleotide-binding oligomerization domain 2)-mediated signaling inhibitor (IC50 = 400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells). Does not affect NOD1, TNFR1, or TLR-2-mediated responses. Also shown to diminish synergy between NOD2 and TLR2. Reduces MDP-stimulated IL-8, IL-6, IL-1β, and TNFα release in primary human monocytes (~5 µM), but does not affect Pam2CSK4-stimulated IL-8 release. Due to a lack of typical activation loop/hinge-binding motif it is unlikely to act as a kinase inhibitor. NOD1 Inhibitor, Nodinitib-1 (Cat. No. 488004) is also available.

          Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
          Catalogue Number533718
          Brand Family Calbiochem®
          SynonymsN-(2-(1-(2-(2,3-Dihydro-1H-inden-5-ylamino)-2-oxoethyl)-1H-benzo[d]imidazol-2-yl)ethyl)-N-methylbenzamide, Nucleotide-binding Oligomerization Domain 2 Signaling Inhibitor II, MDP/NOD2-Mediated Signaling Inhibitor, GSK 717
          DescriptionNOD2 Signaling Inhibitor II, GSK717
          References
          ReferencesRickard, D.J., et al. 2013. PLoS ONE.D40 8, e69619.
          Product Information
          FormWhite solid
          Hill FormulaC₂₈H₂₈N₄O₂
          Chemical formulaC₂₈H₂₈N₄O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetNOD2
          Primary Target IC<sub>50</sub>400 nM for MDP-stimulated IL-8 secretion in HEK293/hNOD2 cells
          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 3 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          NOD2 Signaling Inhibitor II, GSK717 SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Rickard, D.J., et al. 2013. PLoS ONE.D40 8, e69619.
          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.

          Revision23-September-2016 JSW
          SynonymsN-(2-(1-(2-(2,3-Dihydro-1H-inden-5-ylamino)-2-oxoethyl)-1H-benzo[d]imidazol-2-yl)ethyl)-N-methylbenzamide, Nucleotide-binding Oligomerization Domain 2 Signaling Inhibitor II, MDP/NOD2-Mediated Signaling Inhibitor, GSK 717
          DescriptionA cell-permeable benzimidazole diamide compound that selectively inhibits muramyl dipeptide/MDP-induced, nucleotide-binding oligomerization domain 2/NOD2-mediated cytokine production (% inhibiton/cytokine = 91%/IL-8, 89%/IL-6, 87%/IL-1β, 80%/TNFα 25 h post 5 µM drug addition & 24 h post 100 ng/mL MDP stimulation) in primary human monocyte cultures, but not but not TLR2/6 agonist Pam2CSK4- (100 pg/mL) stimulated IL-8 secretion even at concentrations as high as 16 µM. Based on selectivity studies using the less potent, non-N-methylated analog GSK669, GSK717 is not expected to act as a kinase inhibitor or display significant potency against MDP-independent NOD2 activation, TNFα receptor- and NOD1-mediated cytokine productions. A great complement to the NOD1 signaling-selective inhibitor Nodinitib-1 (Cat. No. Cat. No. 488004). The exact mechanism of inhibition is not yet determined.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          Chemical formulaC₂₈H₂₈N₄O₂
          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 3 months at -20°C.
          Toxicity Standard Handling
          ReferencesRickard, D.J., et al. 2013. PLoS ONE.D40 8, e69619.