Kaempferol

Biological Activity

Activates the mitochondrial Ca²⁺ uniporter (EC₅₀ = 7 μM). Induces caspase-9-mediated apoptosis in cancer cell lines via downregulation of polo-like kinase 1 (PLK1) expression. Exhibits antioxidant activity and attenuates osteoclastic bone reabsorption in vitro. Also blocks EGF-induced histone H3Ser¹⁰ phosphorylation in mouse epidermal JB6 C141 cells. Activates transcriptional coactivator with PDZ-binding motif (TAZ) and increases osteoblast differentiation of mesenchymal stem cells while inhibiting adipocyte differentiation. Naturally occurring flavonoid found in Gingko biloba and red wine. Kaempferol has antiviral activity against Japanese encephalitis virus (JEV) in infected BHK21 (EC₅₀ = 21.5 μM). Kaempferol directly inhibits viral replication and protein expression by binding JEV frameshift site RNA (fsRNA). Kaempferol influences frameshift efficiency in virus-infected cells through interfering with a downstream RNA pseudoknot structure. Kaempferol has also been reported to exhibit activity against herpes simplex virus, influenza viruses (H1N1 and H9N2) and hepatitis B virus under in vitro conditions.

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Mycoplasma pneumoniae modulates STAT3-STAT6/EGFR-FOXA2 signaling to induce overexpression of airway mucins.
   Hao Y, Kuang Z, Jing J, Miao J, Mei L, Lee R, Kim S, Choe S, Krause D, Lau G
   Infect Immun, 2014;82(12):5246-55.
2. Ribosomal S6 kinase 2 is a key regulator in tumor promoter induced cell transformation.
   Cho et al.
   Cancer Res., 2007;67:8104
3. Direct activation of the mitochondrial calcium uniporter by natural plant flavonoids.
   Montero et al.
   Biochem.J., 2004;384:19
4. Kaempferol attenuates 2-deoxy-D-ribose-induced oxidative cell damage in MC3T3-E1 osteoblastic cells.
   Suh et al.
   Biol.Pharm.Bull., 2009;32:746
5. Downregulation of PLK-1 expression in kaempferol-induced apoptosis of MCF-7 cells.
   Kang et al.
   Eur.J.Pharmacol., 2009;611:17
6. Modulation of Ca²⁺ release and Ca²⁺ oscillations in HeLa cells and fibroblasts by mitochondrial Ca²⁺ uniporter stimulation.
   Vay et al.
   J.Physiol., 2009;580:39
7. TAZ is required for the osteogenic and anti-adipogenic activities of kaempferol.
   Byun et al.
   Bone, 2012;50:364

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