PIM1

0.34μM(IC₅₀)

PIM2

3.45μM(IC₅₀)

RSK2

2.82μM(IC₅₀)

PKA

21.2μM(IC₅₀)

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.

Quercetagetin also inhibits PIM2, PKA, and RSK2 with IC50s of 3.45, 21.2, and 2.82 µM, respectively[2].Quercetagetin (0.1, 1, 10, and 100 μM, 72 hours) inhibits growth of RWPE2 prostate cancer cells with average ED50 is 3.8 μM[2].

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].

[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.
[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.
[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.