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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).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 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
530655
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
27031-00-1C₁₇H₁₅N₃O₃

Products

Catalogue NumberPackaging Qty/Pack
5306550001 Glass bottle 25 mg
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
Catalogue Number GTIN
5306550001 04055977260427

Documentation

Mitochondrial GPDH Inhibitor, iGP-1 - CAS 27031-00-1 - 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
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.