Merck, 551600-100MG-M, Quercetin, Dihydrate

General description
A cell-permeable and reversible inhibitor of PIM1 kinase (IC₅₀ = 43 nM), PI 3-K (IC₅₀ = 3.8 µM) and phospholipase A₂ (IC₅₀ = 2 µM). Also inhibits mitochondrial ATPase, phosphodiesterases, and protein kinase C. Induces apoptosis in K562, Molt-4, Raji, and MCAS tumor cell lines. Reported to activate sirtuins and promote the survival of eukaryotic cells.
A cell-permeable inhibitor of PIM1 kinase (IC₅₀ = 43 nM), PI 3-K (IC₅₀ = 3.8 µM) and phospholipase A₂ (IC₅₀ = 2 µM). Also inhibits mitochondrial ATPase, phosphodiesterases, and protein kinase C. Induces apoptosis in K562, Molt-4, Raji, and MCAS tumor cell lines. Reported to activate sirtuins and promote the survival of eukaryotic cells.
Biochem/physiol Actions
Primary Target
PI 3-kinase
Target IC₅₀: 43 nM, 3.8 µM, 2 µM against PIM1 kinase, PI 3-K, and phospholipase A2, respectively
Other Notes
Bullock, A.N., et al. 2005. J. Med. Chem.48, 7604.
Howitz, K.T., et al. 2003. Nature425, 191.
Wei, Y.Q., et al. 1994. Cancer Res.54, 4952.
Shibasaki, F., et al. 1993. Biochem. J.289, 227.
Matter, W.F., et al. 1992. Biochem. Biophys. Res. Comm.186, 624.
Levy, J., et al. 1984. Biochem. Biophys. Res. Commun.123, 1227.
Graziani, Y., et al. 1983. Eur. J. Biochem.135, 583.
Gschwendt, M., et al. 1983. Biochem. Biophys. Res. Commun. 117, 444.
Ruckstuhl, M., et al. 1979. Biochem. Pharmacol.28, 535.
Beretz, A., et al. 1978. Experientia 34, 1054.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Toxic & Carcinogenic / Teratogenic (G)