Biochem/physiol Actions

Reversible: yes

Product competes with ATP.

Primary TargetPKC

Target IC₅₀: 10 nM, 17 µM, 900 nM against PKC, CaM kinase II, and protein kinase A, respectively; 6.8 nM against GSK-3 in primary adipocytes; 2.8 nM against GSK-3β immunoprecipitates)

Cell permeable: yes

General description

A cell-permeable, competitive, reversible, and selective inhibitor of protein kinase C (PKC; IC₅₀ = 10 nM) over CaM kinase II (IC₅₀ = 17 µM) and protein kinase A (IC₅₀ = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC₅₀ = 6.8 nM) and in GSK-3β immunoprecipitates (IC₅₀ 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC₅₀ = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells.

A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC; IC₅₀ = 10 nM) over CaM kinase II (IC₅₀ = 17 µM) and protein kinase A (IC₅₀ = 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC₅₀ = 6.8 nM) and in GSK-3β immunoprecipitates (IC₅₀ = 2.8 nM). An inhibitor of MAP kinase phosphatase-1 expression and an activator of JNK1. Inhibits the phosphorylation of Raf-1 and induces apoptosis, independent of its effects on PKC, in HL-60 cells. Also inhibits sirtuin in a NAD-competitive manner (IC₅₀ = 3.5 µM and 0.8 µM for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 µg/181 µl) solution of Ro-31-8220 (Cat. No. 557521) in H₂O is also available.

Legal Information

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

Other Notes

Trapp, J., et al. 2006. J. Med. Chem.In press.Powell, D.J., et al. 2003. Mol. Cell Biol.23, 7794.Han, Z., et al. 2000. Cell Death Differ.7, 521.Hers, I., et al. 1999. FEBS Lett.460, 433.Beltman, J., et al. 1996. J. Biol. Chem. 271, 27018.Keller, H.U., and Niggli, V. 1993. Biochem. Biophys. Res. Commun.194, 1111.McKenna, J.P., and Hanson, P.J. 1993. Biochem. Pharmacol.46, 583.Davis, P.D., et al. 1992. J. Med. Chem. 35, 994.

Packaging

500 µg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.

Warning

Toxicity: Standard Handling (A)