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质量水平
方案
≥97% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
beige
溶解性
DMSO: 100 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
Clc1ccc(cc1)NC(=O)c2cc3c(cc2O)cccc3
InChI
1S/C17H12ClNO2/c18-13-5-7-14(8-6-13)19-17(21)15-9-11-3-1-2-4-12(11)10-16(15)20/h1-10,20H,(H,19,21)
InChI key
OHAXNCGNVGGWSO-UHFFFAOYSA-N
一般描述
在基于 HEK293T 和无细胞海肾荧光素酶(RLuc) 互补测定(IC50 分别为 2.26 和 2.9 M)中,一种细胞可渗透的萘酰胺化合物有效阻断 CBP 的 KIX 结构域和 CREB 的 KID 结构域之间的相互作用。与 CBP′ KIX 结构域结合(Kd ~8.6 M,使用重组 KIX)。研究表明,在基于 HEK293T 的 RLuc 报告基因测定(IC50<2.5 M) 中抑制毛喉素诱导的 CRE-(cAMP 反应元件)依赖性转录活性,而对 KID 非依赖性 CREB-VP16 转录活性几乎没有影响。还报道了抑制萤火虫萤光素酶(IC50 ~1 M)的酶活性,但不抑制 RLuc。
在基于 HEK293T 和无细胞海肾荧光素酶(RLuc) 互补测定(IC50 分别为 2.26 和 2.9 µM)中,一种细胞可渗透的萘酰胺化合物有效阻断 CBP 的 KIX 结构域和 CREB 的 KID 结构域之间的相互作用。与 CBP′ KIX 结构域结合(Kd ~8.6 µM,使用重组 KIX)。研究表明,在基于 HEK293T 的 RLuc 报告基因检测(IC50<2.5 µM) 中抑制由毛喉素(货号 344270)诱导的 CRE-(cAMP 反应元件)依赖性转录活性,而对不依赖 KID 的 CREB-VP16 几乎没有影响转录活性。 还报道了抑制萤火虫萤光素酶(IC50 ~1 µM)的酶活性,但不抑制 RLuc。
包装
用惰性气体包装
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6个月。
其他说明
Li, B.X. and Xiao, X., 2009.ChemBioChem10, 2721.
Best, J.L., et al. 2004.Proc.Natl.Acad.Sci. USA101, 17622.
Best, J.L., et al. 2004.Proc.Natl.Acad.Sci. USA101, 17622.
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
Eye Irrit. 2 - Skin Sens. 1B
储存分类代码
11 - Combustible Solids
WGK
WGK 1
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