推荐产品
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
deep orange
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
N1C(=O)C(=C(C1=O)c4c5c([nH]c4)cccc5)c2c3c([n](c2)CCCN(C)C)cccc3
InChI
1S/C25H24N4O2/c1-28(2)12-7-13-29-15-19(17-9-4-6-11-21(17)29)23-22(24(30)27-25(23)31)18-14-26-20-10-5-3-8-16(18)20/h3-6,8-11,14-15,26H,7,12-13H2,1-2H3,(H,27,30,31)
InChI key
QMGUOJYZJKLOLH-UHFFFAOYSA-N
一般描述
一种高度选择性、细胞可渗透性和可逆的蛋白激酶C（PKC）抑制剂（IC50=10 nM），其结构类似于星形孢菌素。作为PKC的ATP结合位点的竞争性抑制剂。对于PKCα、βI、βII、γ、δ 和 ε 同工酶具有高选择性。有效抑制原代脂肪细胞裂解物（IC50 = 360 nM）和GSK-3β免疫沉淀物（IC50 = 170 nM）中的GSK-3。可能以更高的浓度（IC50 = 2 µM）抑制蛋白激酶A。也可以使用1 mg/mL的双吲哚基马来酰亚胺I（目录编号203293）在无水DMSO中的溶液。
一种高度选择性细胞渗透性蛋白激酶C（PKC）抑制剂（IC50=10 nM），其结构类似于星形孢菌素。作为PKC的ATP结合位点的竞争性抑制剂。对于PKCα、βI、βII、γ、δ 和 ε 同工酶具有高度选择性。可能以更高的浓度（IC50 = 2 µM）抑制蛋白激酶A。还抑制槲皮素、H-89或除草霉素A处理的NPC-076细胞中的端粒酶活性。
生化/生理作用
主要靶标
PKC
PKC
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标IC50：针对蛋白激酶C（PKC），为10 nM；分别针对原代脂肪细胞裂解物的和GSK-3β免疫沉淀物中的GSK-3，为360 nM和170 nM
警告
毒性：标准处理（A）
制备说明
仅在使用前再用水相缓冲液进行稀释。
重悬
复溶后，等分并冷冻保存（-20°C）。DMSO储备液可在-20°C下稳定保存4个月。
其他说明
Hers, I., et al. 1999.FEBS Lett.460, 433.
Ku, W.-C., et al. 1997.Biochem.Biophys.Res. Commun.241, 730.
Gekeler, V., et al. 1996.Br. J. Cancer 74, 897.
Kiss, Z., et al. 1995.Biochim.Biophys.Acta 1265, 93.
Toullec, D., et al. 1991.J. Biol. Chem. 266, 15771.
Ku, W.-C., et al. 1997.Biochem.Biophys.Res. Commun.241, 730.
Gekeler, V., et al. 1996.Br. J. Cancer 74, 897.
Kiss, Z., et al. 1995.Biochim.Biophys.Acta 1265, 93.
Toullec, D., et al. 1991.J. Biol. Chem. 266, 15771.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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