产品说明

一般描述

Ro 31-8220是星形孢菌素的一种双吲哚基马来酰亚胺衍生物。Ro 31-8220可阻断MAP激酶磷酸酶-1(MKP-1)的表达、诱导c-Jun表达并刺激Jun N末端激酶(JNK1)。它具有免疫抑制特性。

包装

1, 5 mg in glass bottle

生化/生理作用

抑制GRK-5(G蛋白偶联受体激酶)；PKC(蛋白激酶C)；MAPKAP激酶1β及p70 S6激酶。

特点和优势

该化合物在受体分类和信号转导手册中GRK、GSK-3、 MAPKAP以及PKC页面中进行了详细介绍。如需浏览其他手册页，请点击此处。
这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

注意

光敏性

基本信息

产品性质

安全信息

产品说明

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 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.
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.

包装

500 μg in Plastic ampoule

生化/生理作用

Cell permeable: yes
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)
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

基本信息

产品性质

安全信息