Antitumoral Quinol1h Small Molecule (Tool Compound)

A new class of molecule (4-hydroxy-4-hetarylcyclohexa-2,5-dien-1-ones) bearing a new pharmacophore (quinols’) with potent activity against renal, colon and breast cell lines in the NCI 60-cell panel.

Contributors

Inventor Institute
Malcolm F G Stevens University of Nottingham
Cat. #: 151834
Tool sub type: Antitumoral
Research Fields: Cell biology;Genetics
Application: Antitumor activity observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM), and in breast cancer cell lines. Potent inhibitory effect in NCI 60 cells (GI50 =16 nM and LC50 = 2.24 ÂľM).
Product description: A new class of molecule (4-hydroxy-4-hetarylcyclohexa-2,5-dien-1-ones) bearing a new pharmacophore (quinols') has been identified with potent activity against renal, colon and breast cell lines in the NCI 60-cell panel.
Additional notes: Exhibits a mean GI50 value of 16 nM and a mean LC50 value of 2.24 uM in the NCI 60- cell-line screen, with LC50 activity in the HCT 116 human colon cancer cell line below 10 nM. Compound available for screening or similar studies. For larger quantities (>20mg) please contact Ximbio.
Molecular weight: 383.4
Primary target: Thioredoxin reductase
Storage conditions: -20° C (desiCating conditions)
Shipping conditions: Dry Ice
Solubility: DMSO to 100 mM
References:

Chew et al. 2008. FASEB J. 22(6):2072-83. PMID: 18180330.

Thioredoxin reductase inhibition by antitumor quinols: a quinol pharmacophore effect correlating to antiproliferative activity.

Berry et al. 2005. J Med Chem. 48(2):639-44. PMID: 15658878.

Quinols as novel therapeutic agents. 2.(1) 4-(1-Arylsulfonylindol-2-yl)-4-hydroxycyclohexa-2,5-dien-1-ones and related agents as potent and selective antitumor agents.

Wells et al. 2003. J Med Chem. 46(4):532-41. PMID: 12570375.

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