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530655 Mitochondrial GPDH Inhibitor, iGP-1 - CAS 27031-00-1 - Calbiochem

A cell-permeable, potent, selective, and dose-dependent inhibitor of mitochondrial, but not cytosolic, sn-glycerol-3-phosphate dehydrogenase (IC₅₀ against mGPDH = 6.3 µM).

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Synonymes: N-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1, iGP1

Primary Target: mGPDH
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530655
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Tableau de caractéristiques principal

CAS #Empirical Formula
27031-00-1C₁₇H₁₅N₃O₃

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      Description
      OverviewA cell-permeable benzimidazolyl-phenylamidosuccinate compound that acts as a potent, selective, and dose-dependent inhibitor against mitochondrial, but not cytosolic, sn-glycerol-3-phosphate dehydrogenase (IC50 against mGPDH = 6.3 µM). Shown to directly interact with a single, allosteric binding site on mGPDH and displays mixed type of inhibition kinetics (Kic = 9.5 µM and Kiu = 14.6 µM, glycerol phosphate/GP-competitive against free and GP-uncompetitive against GP-bound mGPDH). Reduces H2O2 production by IQ site (IC50 = 13.6 µM) and inhibits ΔΨm driven by low concentrations of succinate (0.5 µM), but does not inhibit glutamate-, malate-, pyruvate-, or palmityoylcarnitine-driven ΔΨm. Does not prevent pyruvate uptake into cells or mitochondria and has no direct effect on Glycolysis in synaptosomes.
      Catalogue Number530655
      Brand Family Calbiochem®
      SynonymsN-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1, iGP1
      References
      ReferencesOrr, A.L., et al. 2014. PLoS One 9, e89938.
      Product Information
      CAS number27031-00-1
      FormBeige solid
      Hill FormulaC₁₇H₁₅N₃O₃
      Chemical formulaC₁₇H₁₅N₃O₃
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetmGPDH
      Primary Target IC<sub>50</sub>6.3 µ
      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
      Référence GTIN
      5.30655.0001 04055977260427

      Documentation

      Mitochondrial GPDH Inhibitor, iGP-1 - CAS 27031-00-1 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Orr, A.L., et al. 2014. PLoS One 9, e89938.
      Fiche technique

      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.

      Revision12-June-2014 JSW
      SynonymsN-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1, iGP1
      DescriptionA cell-permeable thiadiazolyl-butyl-pyridazinyl compound that displays increased fluorescence with acidified pH (by 8-fold from pH 7.0 to 1.5; Ex 342 nm & Em 378 nm) and selectively inhibits mitochondrial sn-glycerol 3-phosphate (GP) dehydrogenase (mGPDH) activity (IC50 = 6.3 µM by DCPIP assay using rat skeletal muscle mitochondria preparation with 1 µ Ca2+), but not cytosolic GPDH (up to 80 µM using rabbit cGPDH), by targeting free mGPDH in a GP-competitive manner (KicKiu2-dependent complex I activity and little potency toward unbiquinol/QH2-dependent complex III activity, nor FMN-dependent complex I or II activity. Under conditions where Lactate dehydrogenase-mediated NAD+ generation is blocked by Oxamate in murine cortical synaptosome preparations, a small but significant dependence on mGPDH-mediated GP shuttle for NAD+ generation to support the high glycolytic demand for pyruvate generation from glucose (15 mM) is reported, as evidenced by a more pronounced mitochondrial respiration inhibition in the presence of FCCP and Oligomycin (4 µg/mL; Cat. No. 495455) with the combined treatment of 0.5 mM aminooxyacetate (AOA) and 100 µM iGP-1 than with AOA alone.
      FormBeige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number27031-00-1
      Chemical formulaC₁₇H₁₅N₃O₃
      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
      ReferencesOrr, A.L., et al. 2014. PLoS One 9, e89938.