328007
ERK抑制剂II，FR180204
ERK Inhibitor II, FR 180204, CAS 865362-74-9, is a cell-permeable, potent, ATP-competitive inhibitor of ERK1 and ERK2 (IC₅₀ = 510 nM and 330 nM; Ki = 310 nM and 140 nM, respectively).
别名:
ERK抑制剂II，FR180204, 5-(2-苯基-吡唑并[1,5-a]吡啶-3-基)-1H-吡唑并[3,4-c]哒嗪-3-基胺
质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
yellow
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C18H13N7/c19-17-12-10-13(20-22-18(12)23-21-17)15-14-8-4-5-9-25(14)24-16(15)11-6-2-1-3-7-11/h1-10H,(H3,19,21,22,23)
InChI key
XVECMUKVOMUNLE-UHFFFAOYSA-N
一般描述
一种细胞可渗透性吡唑并哒嗪胺，可作为ERK1和ERK2的有效，ATP竞争性抑制剂（IC50分别为510 nM和330 nM；Ki分别为310 nM和140 nM）。选择性比p38高约20倍α（IC50 = 10 µM），对IKKα、MEK1、MKK4、PDGFRα、PKCα、Src和Syk几乎没有活性，即使在浓度高达30 µM时也是如此。在Mv1Lu上皮细胞中显示出抑制TGFβ−-诱导的AP-1活化的作用（IC50为3.1 µM）。也可用ERK抑制剂II，阴性对照（目录编号328008）。 也可以10 mM的DMSO溶液（目录号328010）提供。
一种细胞可渗透性吡唑并哒嗪胺，可作为ERK1和ERK2的有效，ATP竞争性抑制剂（IC50分别为510 nM和330 nM；Ki分别为310 nM和140 nM）。选择性比p38高约20倍α（IC50 = 10 µM），对IKKα、MEK1、MKK4、PDGFRα、PKCα、Src和Syk几乎没有活性，即使在浓度高达30 µM时也是如此。在Mv1Lu上皮细胞中显示出抑制TGFβ−-诱导的AP-1活化的作用（IC50为3.1 µM）。也可用ERK抑制剂II，阴性对照（目录编号328008）。也可提供InSolution形式（目录号328010）。
生化/生理作用
主要靶标
ERK1和ERK2
ERK1和ERK2
产物与ATP竞争。
可逆：否
细胞可渗透性：是
靶标IC50：510 nm和330 nm
靶标Ki：310 nM和140 nM，分别针对ERK1和ERK2
包装
用惰性气体包装
制备说明
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
Ohori, M., et al. 2005.Biochem.Biophys.Res. Commun.336, 357.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：标准处理（A）
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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