Kaempferol

A cell-permeable phytoestrogen that inhibits topoisomerase I-catalyzed DNA religation in HL-60 cells. Offers protection against Aβ_25-35-induced cell death in neonatal cortical neurons. Its protective effects are comparable to that of estradiol. Blocks the Aβ-induced activation of caspase-2, -3, -8, and -9, and reduces NMDA-induced neuronal apoptosis. Reported to be a potent inhibitor of monoamine oxidases. Acts as an inhibitor of COX-1 activity (IC₅₀ = 180 µM), and of transcriptional activation of COX-2 (IC₅₀<15 µM).

A cell-permeable, phytoestrogen that offers protection against Aβ_25-35-induced cell death in neonatal cortical neurons. Its protective effects are comparable to that of estradiol. Reduces the activation of caspases 2, 3, 8, and 9 by Aβ. Inhibits topoisomerase I-catalyzed DNA religation in HL-60 cells. Also shown to protect against NMDA-induced neuronal toxicity in vitro in cultured rat cortical neurons. Acts as an inhibitor of cyclooxygenases (COX-1, IC₅₀ = 180 µM) and COX-2 (IC₅₀ = ~15 µM).

Cell permeable: yes

Primary Target
Topoisomerase I-catalyzed DNA religation in HL-60 cells

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 180 µM against COX-1 activity

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Wang, C.N., et al. 2001. J. Biol. Chem.276, 5287.
Sloley, B.D., et al. 2000. J. Pharm. Pharmacol.52, 451.
Wang, H., et al. 2000. Phytomedicine7, 15.
Liang, Y.C., et al. 1999. Carcinogenesis20, 1945.
Roth, A., et al. 1999. J. Neurosci. Res.57, 399.
Boege, F., et al. 1996. J. Biol. Chem.271, 2262.
Constantinou, A., et al. 1995. J. Nat. Prod.58, 217.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Carcinogenic / Teratogenic (D)