merck millipore,默克密理博,557520,Ro-31-8220 - CAS 138489-18-6

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merck millipore,默克密理博,557520,Ro-31-8220 - CAS 138489-18-6 - Calbiochem
产品名称：Ro-31-8220 - CAS 138489-18-6 - Calbiochem
产品型号：557520
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).

merck millipore,默克密理博,557520,Ro-31-8220 - CAS 138489-18-6 - Calbiochem

产品介绍

merck millipore,默克密理博,557520,Ro-31-8220 - CAS 138489-18-6 - Calbiochem

重要规格表

经验配方	CAS号
C₂₅H₂₃N₅O₂S · CH₄O₃S	138489-18-6

描述
概述	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.
产品目录编号	557520
品牌系列	Calbiochem®
同义词	3-[1-[3-(Amidinothio)propyl-1H-indol-3-yl]-3-(1-methyl-1H-indol-3-yl)maleimide, Bisindolylmaleimide IX, Methanesulfonate

参考
参考	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.

参考

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.

产品信息
CAS号	138489-18-6
具有ATP竞争性	Y
形式	Red solid
Hill配方	C₂₅H₂₃N₅O₂S · CH₄O₃S
化学配方	C₂₅H₂₃N₅O₂S · CH₄O₃S
Molar Mass	553.7
吸湿	Hygroscopic
可逆	Y
结构配方图像

生物信息
主靶	PKC
主靶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)
纯度	≥95% by HPLC

理化信息
细胞可渗透	Y
溶解度	DMSO or H₂O

储存和货运信息
货运代码	Ambient Temperature Only
毒性	Standard Handling
储存	+2°C to +8°C
避光	Protect from light
吸湿	Hygroscopic
无需冷冻	No
特殊指南	Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 4 months at -20°C.