Biochem/physiol Actions

Primary TargethFKBP12

General description

Antifungal antibiotic that does not inhibit several species of pathogenic bacteria at 100 µg/ml. Inhibits protein synthesis in eukaryotes but not in prokaryotes. Interacts directly with the translocase enzyme, interfering with the translocation step. Inhibits cell-free protein synthesis in eukaryotes. Competitively inhibits hFkBP12 (K_i = 3.4 µM). Triggers apoptosis in HL-60 cells, T-cell hybridomas, Burkitt′s lymphoma cells, and a variety of other cell types, including rodent macrophages. Inhibits DNA cleavage in rat thymocytes treated with thapsigargin, methylprednisolone, and ionomycin. Rapidly destroyed in alkaline solutions.

Antifungal antibiotic that inhibits protein synthesis in eukaryotes but not in prokaryotes. Interacts directly with the translocase enzyme, interfering with the translocation step. Inhibits cell-free protein synthesis in eukaryotes. Competitively inhibits hFKBP12 (K_i = 3.4 µM). Triggers apoptosis in HL-60 cells, T cell hybridomas, Burkitt's lymphoma cells, and a variety of other cell types including rodent macrophages. However, it inhibits DNA cleavage in rat thymocytes treated with Thapsigargin (Cat. No. 586005), methylprednisolone, and Ionomycin (Cat. Nos. 407950 and 407952). Rapidly destroyed in alkaline solutions. Also available as a 300 mM solution in DMSO (Cat. No. 508739).

Legal Information

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

Other Notes

Christner, C., et al. 1999. J. Med. Chem. 42, 3615.Lu, Q., et al. 1996. Arch. Biochem. Biophys.334, 175.Chow, S.C., et al. 1995. Exp. Cell Res.216, 149.Cotter, T.G., et al. 1992. Anticancer Res.12, 773.Takano, Y.S., et al. 1991. J. Pathol.163, 329.Waring, P. 1990. J. Biol. Chem. 265, 14476.

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Packaging

100 mg in Glass bottle

1 g in Alu drum

Reconstitution

Following reconstitution, aliquot and freeze (-20°C) for long term storage or refrigerate (4°C) for short term storage. Stock solutions are stable for up to 6 weeks at 4°C, pH 3-5.

Warning

Toxicity: Highly Toxic & Carcinogenic / Teratogenic (I)