Uses
Quercetagetin (6-Hydroxyquercetin) is a flavonoid[1]. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM)[2]. Anti-inflammatory and anticancer properties.
Definition
ChEBI: A hexahydroxyflavone that is flavone substituted by hydroxy groups at positions 3, 5, 6, 7, 3' and 4' respectively.
Biological Activity
Cell permeable: yes', 'Primary Target
PIM1 kinase', 'Product competes with ATP.', 'Reversible: yes', 'Target IC50: 340 nM against PIM1 kinase
in vivo
Quercetagetin significantly inhibits UVB-induced skin cancer development. Topical application of 4 or 20 nmol of Quercetagetin to mouse skin reduces tumor incidence by 32.0% and 46.7%, respectively[3].
| Animal Model: | SKH-1 hairless mice model[3] |
| Dosage: | 4 or 20 nmol |
| Administration: | Topical application; 28 weeks |
| Result: | Inhibited UVB-induced skin tumorigenesis in SKH-1 hairless mice models. Delayed the development of tumors and reduced tumor volumes in an SKH-1 hairless mice model. |
IC 50
PIM1: 0.34 μM (IC
50); PIM2: 3.45 μM (IC
50); RSK2: 2.82 μM (IC
50); PKA: 21.2 μM (IC
50)
References
[1] Yang X, et al. Isolation and identification of an antioxidant flavonoid compound from citrus-processing by-product. J Sci Food Agric. 2011 Aug 15;91(10):1925-7. DOI:
10.1002/jsfa.4402[2] Holder S, et al. Characterization of a potent and selective small-molecule inhibitor of the PIM1 kinase. Mol Cancer Ther. 2007 Jan;6(1):163-72. DOI:
10.1158/1535-7163.MCT-06-0397[3] Baek S, et al. Structural and functional analysis of the natural JNK1 inhibitor quercetagetin. J Mol Biol. 2013 Jan 23;425(2):411-23. DOI:
10.1016/j.jmb.2012.10.019
