Cat. #151834
Antitumoral Quinol1h Small Molecule (Tool Compound)
Cat. #: 151834
Sub-type: Antitumoral
Availability: Please enquire for quantities and pricing
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).
This fee is applicable only for non-profit organisations. If you are a for-profit organisation or a researcher working on commercially-sponsored academic research, you will need to contact our licensing team for a commercial use license.
Contributor
Inventor: Malcolm F G Stevens
Institute: University of Nottingham
Tool Details
*FOR RESEARCH USE ONLY
- Tool name: Antitumoral Quinol1h Small Molecule (Tool Compound)
- Molecular formula: C20H14FNO4S
- Tool sub type: Antitumoral
- Primary target: Thioredoxin reductase
- 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.
- 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).
- Iupac: 4-(1-Benzenesulfonyl-6-fluoro-1Hindol-2-yl)-4-hydroxy-cyclohexa-2,5-dienone
- Molecular weight: 383.4
- Solubility: DMSO to 100 mM
- 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.
Handling
- Purity: 383.4 g/mol
- Storage conditions: -20° C (desiCating conditions)
- Shipping conditions: Dry Ice
Target Details
- Primary target: Thioredoxin reductase
Application Details
- 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).
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.
- 4-Substitut...
