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

533966
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₆H₁₀F₃NO₃ 1269802-68-7

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      5.33966.0001
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          Glass bottle 10 mg
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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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Maftouh, M., et al. 2014. Br. J. Cancer. 110, 172.
          Granchi, C., et al. 2011. J. Med. Chem. 54, 1599.
          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.

          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 +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
          ReferencesMaftouh, M., et al. 2014. Br. J. Cancer. 110, 172.
          Granchi, C., et al. 2011. J. Med. Chem. 54, 1599.