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533966 LDH-A Inhibitor III, NHI-1 - CAS 1269802-68-7 - Calbiochem

A cell-permeable, both NADH and pyruvate-competitive isoform A-selective LDH inhibitor. Exhibits enhanced anticancer activity under hypoxic conditions.

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Synonymes: 1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylic acid, Lactate Dehydrogenase A Inhibitor III, LDH-M Inhibitor III

Primary Target: LDH-A/LDH-1
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533966
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Tableau de caractéristiques principal

CAS #Empirical Formula
1269802-68-7C₁₆H₁₀F₃NO₃

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      Description
      OverviewA cell-permeable, non-cytotoxic N-hydroxyindole (NHI) carboxylate that acts as a potent, reversible, and isoform selective inhibitor of lactic dehydrogenase (LDH) A/LDH-1. Inhibition appears to be competitive with respect to both pyruvate (Ki = 4.7 µM) and NADH (cofactor; Ki = 8.9 µM). Acts by occupying the whole substrate pocket and part of the cofactor pocket of LDH-A. Blocks the growth of various cancer cell lines by causing an arrest at G1 phase and inducing apoptosis (IC50 = 10.8, 10.6, 11.4, and 31.5 µM for A2780/cOHP, MSTO-211H, NIH-H28, and H630 cells, respectively). Exhibits enhanced anticancer activity under hypoxic conditions (GI50 = 0.90 µM/hypoxia vs. 16.3 µM/normoxia in LPC006 cultures) and strongly synergizes with gemcitabine (Cat. No. 504594).

      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 Number533966
      Brand Family Calbiochem®
      Synonyms1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylic acid, Lactate Dehydrogenase A Inhibitor III, LDH-M Inhibitor III
      References
      ReferencesMaftouh, M., et al. 2014. Br. J. Cancer. 110, 172.
      Granchi, C., et al. 2011. J. Med. Chem. 54, 1599.
      Product Information
      CAS number1269802-68-7
      FormOff-white solid
      Hill FormulaC₁₆H₁₀F₃NO₃
      Chemical formulaC₁₆H₁₀F₃NO₃
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetLDH-A/LDH-1
      Primary Target IC<sub>50</sub>10.8, 10.6, 11.4, and 31.5 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 3 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
      5339660001 04055977281651

      Documentation

      LDH-A Inhibitor III, NHI-1 - CAS 1269802-68-7 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Maftouh, M., et al. 2014. Br. J. Cancer. 110, 172.
      Granchi, C., et al. 2011. J. Med. Chem. 54, 1599.
      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.

      Revision26-June-2017 JSW
      Synonyms1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylic acid, Lactate Dehydrogenase A Inhibitor III, LDH-M Inhibitor III
      DescriptionA cell-permeable, noncytotoxic NHI (N-hydroxyindole) carboxylate that acts as an isoform A-selective LDH inhibitor (87% inhibition of hLDH-A4 vs 11% inhibition of hLDH-B4 at 125 µM; [NADH] = 25 µM & [pyruvate] = 2 mM) in a competitive manner with respect to both NADH (Ki = 8.9 µM; [pyruvate] = 2 mM) and pyruvate (Ki = 4.7 µM; [NADH] = 200 µM). Shown to effectively inhibit de novo D-[1,6-13C2] glucose-derived lactate production in HeLa cultures (80% and <5% of control Lac/Glu ratio in 12 h, respectively, with 400 and 500 µM inhibitor) and exhibit enhanced anticancer activity under hypoxic conditions (GI50 by SRB assays = 0.90 µM/hypoxia vs. 16.3 µM/normoxia in LPC006 cultures), while diplaying little antiproliferation activity toward non-tumorigenic hTERT-HPNE (ductal pancreatic) and Hs27 (skin fibroblast) even at concentrations as high as 100 µM;.
      FormOff-white solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1269802-68-7
      Chemical formulaC₁₆H₁₀F₃NO₃
      Purity≥98% by HPLC
      SolubilityDMSO (100 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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesMaftouh, M., et al. 2014. Br. J. Cancer. 110, 172.
      Granchi, C., et al. 2011. J. Med. Chem. 54, 1599.