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Merck
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Documentos Principais

681679-M

Millipore

Iron Chelator IV, 21H7

The Iron Chelator IV, 21H7 controls the biological activity of iron-regulated enzymes. This small molecule/inhibitor is primarily used for Cancer applications.

Sinônimo(s):

Iron Chelator IV, 21H7, 6-Bromo-Nʹ-(2-hydroxybenzylidene)-2-methylquinoline-4-carbohydrazide

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About This Item

Fórmula empírica (Notação de Hill):
C18H14BrN3O2
Peso molecular:
384.23
Código UNSPSC:
12352200

Nível de qualidade

Ensaio

≥97% (HPLC)

Formulário

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

off-white

solubilidade

DMSO: 5 mg/mL, light yellow

temperatura de armazenamento

2-8°C

Descrição geral

A cell-permeable salicylaldehyde-acylhydrazone iron chelator that is 20-times more efficient than DFO/desferrioxamine (Cat. No. 252750) in depleting intracellular iron in colon cancer SW480 cells. Iron chelators exert their biological activities by affecting iron-regulated enzymes and singaling events, including HIF1α transcription activation (Effective [21H7] = 10 µM in SW480 and DLD-1 cells) due to inhibition of PHD- (prolyl hydroxylase) mediated HIF1α degradation, as well as stalling and enhancing, respectively, Ferritin and TfRI (Transferrin Receptor I) mRNA translation (Effective [21H7] = 10 µM in SW480 cells) due to iron depletion-induced IRP (Iron Regulatory Protein) IREs (Iron Response Elements) binding. Iron depletion is also reported to inhibit the growths of colorectal adenocarcinoma cultures, DLD-1 (IC50 = 0.6 and 2.9 µM, respectively, by 21H7 and DFO) and SW480 (IC50 = 1.0 and 3.8 µM, respectively, by 21H7 and DFO), as a result of Wnt signaling pathway blockage (Effective conc. = 5 µM 21H7 or 100 µM DFO).
A cell-permeable salicylaldehyde-acylhydrazone iron chelator that is 20-times more efficient than DFO/desferrioxamine (Cat. No. 252750) in depleting intracellular iron in colon cancer SW480 cells. Iron chelators exert their biological activities by affecting iron-regulated enzymes and singaling events, including HIF1α transcription activation due to inhibition of PHD- (prolyl hydroxylase) mediated HIF1α degradation, as well as altered mRNA translations due to enhanced IRP (Iron Regulatory Protein) IREs (Iron Response Elements) binding. Cellular iron depletion is also reported to inhibit the growths of colorectal adenocarcinoma cultures, DLD-1 (IC50 = 0.6 and 2.9 µM, respectively, by 21H7 and DFO) and SW480 (IC50 = 1.0 and 3.8 µM, respectively, by 21H7 and DFO), as a result of Wnt signaling pathway blockage (Effective conc. = 5 µM 21H7 or 100 µM DFO).

Advertência

Toxicity: Standard Handling (A)

Nota de preparo

Slight warming (45°C) is required for complete solubilization.

Outras notas

Song, S., et al. 2011. Cancer Res.71, 7628.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Código de classe de armazenamento

11 - Combustible Solids

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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