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
经验(实验)分子式 | C25H23N5O2S · xCH4O3S |
分子量 | 457.55 (free base basis) |
产品性质
质量水平 | 100 |
测定 | ≥95% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
颜色 | red |
溶解性 | water: 1 mg/mL DMSO: 100 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
安全信息
储存分类代码 | 11 - Combustible Solids |
WGK | WGK 2 |
闪点(F) | Not applicable |
闪点(C) | Not applicable |