Ro-31-8220-CAS 138489-18-6-Calbiochem

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一般描述

A cell-permeable, reversible, competitive, and selective inhibitor of protein kinase C (PKC; IC₅₀= 10 nM) over CaM kinase II (IC₅₀= 17 ?M) 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 ?M and 0.8 ?M for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells. A 5 mM (500 ?g/181 ?l) solution of Ro-31-8220 (Cat. No. 557521) in H₂O is also available.
A cell-permeable, competitive, reversible, and selective inhibitor of protein kinase C (PKC; IC₅₀= 10 nM) over CaM kinase II (IC₅₀= 17 ?M) and protein kinase A (IC₅₀= 900 nM). Potently inhibits GSK-3 in primary adipocytes (IC₅₀= 6.8 nM) and in GSK-3β immunoprecipitates (IC₅₀2.8 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 ?M and 0.8 ?M for SIRT1 and SIRT2, respectively), and induces hyperacetylation of tubulin in A549 cells.

包装

500 μg in Plastic ampoule

生化/生理作用

Cell permeable: yes
Target IC₅₀: 10 nM, 17 ?M, 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)
Product competes with ATP.
Reversible: yes
Primary Target
PKC

警告

Toxicity: Standard Handling (A)

重悬

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

其他说明

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.

法律信息

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

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