533966 Sigma-AldrichLDH-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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Synonyme: 1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylic acid, Lactate Dehydrogenase A Inhibitor III, LDH-M Inhibitor III
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Übersicht
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Key Spec Table
| CAS # | Empirical Formula |
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| 1269802-68-7 | C₁₆H₁₀F₃NO₃ |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
|---|---|---|---|---|---|---|
| 5.33966.0001 |
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Glasflasche | 10 mg |
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| Description | |
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| Overview | A 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 Number | 533966 |
| Brand Family | Calbiochem® |
| Synonyms | 1-Hydroxy-6-phenyl-4-trifluoromethyl-1H-indole-2-carboxylic acid, Lactate Dehydrogenase A Inhibitor III, LDH-M Inhibitor III |
| References | |
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| References | Maftouh, M., et al. 2014. Br. J. Cancer. 110, 172. Granchi, C., et al. 2011. J. Med. Chem. 54, 1599. |
| Product Information | |
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| CAS number | 1269802-68-7 |
| Form | Off-white solid |
| Hill Formula | C₁₆H₁₀F₃NO₃ |
| Chemical formula | C₁₆H₁₀F₃NO₃ |
| Reversible | Y |
| Quality Level | MQ100 |
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| Biological Information | |
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| Primary Target | LDH-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 | |
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| Cell permeable | Y |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Bestellnummer | GTIN |
| 5.33966.0001 | 04055977281651 |
Documentation
LDH-A Inhibitor III, NHI-1 - CAS 1269802-68-7 - Calbiochem SDB
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Literatur
| Übersicht |
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| Maftouh, M., et al. 2014. Br. J. Cancer. 110, 172. Granchi, C., et al. 2011. J. Med. Chem. 54, 1599. |