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530655 Mitochondrial GPDH Inhibitor, iGP-1 - Calbiochem

530655
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₁₅N₃O₃

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      Glass bottle 25 mg
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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®
      SynonymsiGP1, N-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1
      References
      ReferencesOrr, A.L., et al. 2014. PLoS One 9, e89938.
      Product Information
      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

      Documentation

      Mitochondrial GPDH Inhibitor, iGP-1 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Orr, A.L., et al. 2014. PLoS One 9, e89938.
      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.

      Revision12-June-2014 JSW
      SynonymsiGP1, N-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1
      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
      Chemical formulaC₁₇H₁₅N₃O₃
      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
      ReferencesOrr, A.L., et al. 2014. PLoS One 9, e89938.