推荐产品
质量水平
方案
≥95% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
clear
溶解性
DMSO: 200 mg/mL
ethanol: 50 mg/mL
运输
ambient
储存温度
−20°C
InChI key
QFJCIRLUMZQUOT-UQKHEJQMSA-N
一般描述
抗真菌剂和免疫抑制剂。选择性抑制哺乳动物雷帕霉素靶蛋白(mTOR)，并阻断随后的p70 S6激酶激活(IC50 = 50 pM)。可特异性抑制mTORC1，但可磷酸化Akt（蛋白激酶B）Ser473位的mTORC2则对雷帕霉素不敏感。防止 IGF-II 的翻译激活。还防止静止的T细胞进入细胞周期，但不直接阻止细胞周期进程。研究表明，可抑制随后的信号传导事件，例如p110Rb 磷酸化、p34cdc2激酶激活和细胞周期蛋白A合成。表现出与FK-50 6结合蛋白的强结合力。还据报道在鼠B细胞系中诱导凋亡，抑制淋巴因子诱导的细胞增殖（在G1期），并不可逆地阻滞酿酒酵母细胞（在G1）。另提供5 mM (500 µg/109 µl)雷帕霉素DMSO溶液（货号 553211）和10 mM (1 mg/109 µl)雷帕霉素乙醇溶液（货号553212）。
选择性抑制哺乳动物雷帕霉素靶蛋白(mTOR)，并阻断随后的p70 S6激酶激活(IC50 = 50 pM)。可特异性抑制mTORC1，但可磷酸化Akt（蛋白激酶B）Ser473位的mTORC2则对雷帕霉素不敏感。防止 IGF-II 的翻译激活。还防止静止的T细胞进入细胞周期，但不直接阻止细胞周期进程。研究表明，可抑制随后的信号传导事件，例如p110Rb 磷酸化、p34cdc2激酶激活和细胞周期蛋白A合成。表现出与FK-50 6结合蛋白的强结合力。还据报道在鼠B细胞系中诱导凋亡，抑制淋巴因子诱导的细胞增殖（在G1期），并不可逆地阻滞酿酒酵母细胞（在G1期）。
生化/生理作用
主靶
雷帕霉素（mTOR）的哺乳动物靶标
雷帕霉素（mTOR）的哺乳动物靶标
产物不与ATP竞争。
可逆：否
细胞渗透性：否
靶标IC50：50 pM，抑制p70 S6激酶
警告
毒性：标准处理（A）
重悬
复溶后，等分并冷冻保存（-20°C）。储备溶液在-20°C下可稳定保存至多3个月。
其他说明
Chen, T., et al. 2011.Aging Cell.10, 908.
Powell, D.J., et al. 2003.Mol. cell Biol.23, 7794.
Braun, W., et al. 1995.FASEB J.9, 63.
Nielsen, F.C., et al. 1995.Nature 377, 358.
Aagaard-Tillery, K.M. and Jelinek, D.F.1994.Cell.Immunol. 156, 493.
Gottschalk, A.R., et al. 1994.Proc.Natl.Acad.Sci. USA91, 7350.
Morice, W.G., et al. 1993.J. Biol. Chem.268, 3734.
Terada, N., et al. 1993.J. Biol. Chem.268, 12062.
Kuo, J., et al. 1992.Nature 358, 70.
Price, D.J., et al. 1992.Science257, 973.
Heitman, J., et al. 1991.Science253, 905.
Kay, J.E., et al. 1991.Immunology72, 544.
Schreiber, S.L.1991.Science251, 283.
Bierer, B.E., et al. 1990.Proc.Natl.Acad.Sci. USA87, 9231.
Dumont, F.J., et al. 1990.J. Immunol.144, 251.
Powell, D.J., et al. 2003.Mol. cell Biol.23, 7794.
Braun, W., et al. 1995.FASEB J.9, 63.
Nielsen, F.C., et al. 1995.Nature 377, 358.
Aagaard-Tillery, K.M. and Jelinek, D.F.1994.Cell.Immunol. 156, 493.
Gottschalk, A.R., et al. 1994.Proc.Natl.Acad.Sci. USA91, 7350.
Morice, W.G., et al. 1993.J. Biol. Chem.268, 3734.
Terada, N., et al. 1993.J. Biol. Chem.268, 12062.
Kuo, J., et al. 1992.Nature 358, 70.
Price, D.J., et al. 1992.Science257, 973.
Heitman, J., et al. 1991.Science253, 905.
Kay, J.E., et al. 1991.Immunology72, 544.
Schreiber, S.L.1991.Science251, 283.
Bierer, B.E., et al. 1990.Proc.Natl.Acad.Sci. USA87, 9231.
Dumont, F.J., et al. 1990.J. Immunol.144, 251.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
警示用语：
Warning
危险声明
危险分类
Carc. 2 - Repr. 2
储存分类代码
11 - Combustible Solids
WGK
WGK 2
法规信息
监管及禁止进口产品
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