3,3',4',5,6,7-HEXAHYDROXYFLAVONE

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.

ChEBI: A hexahydroxyflavone that is flavone substituted by hydroxy groups at positions 3, 5, 6, 7, 3' and 4' respectively.

Cell permeable: yes', 'Primary Target
PIM1 kinase', 'Product competes with ATP.', 'Reversible: yes', 'Target IC50: 340 nM against PIM1 kinase

PIM1: 0.34 μM (IC₅₀); PIM2: 3.45 μM (IC₅₀); RSK2: 2.82 μM (IC₅₀); PKA: 21.2 μM (IC₅₀)

[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