跳转至内容
Merck
CN

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

登录 查看组织和合同定价。

选择尺寸

关于此项目

经验公式（希尔记法）:
C18H13N7
化学文摘社编号:
865362-74-9
分子量:
327.34
UNSPSC Code:
12352200
MDL number:
MFCD14585805

主要文件

查看所有文档
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助
技术服务
需要帮助？我们经验丰富的科学家团队随时乐意为您服务。
让我们为您提供帮助

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

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

yellow

solubility

DMSO: 10 mg/mL

shipped in

ambient

Quality Level

100

General description

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）。

Biochem/physiol Actions

主要靶标
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

Packaging

用惰性气体包装

Preparation Note

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。

Other Notes

Ohori, M., et al. 2005.Biochem.Biophys.Res. Commun.336, 357.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

毒性：标准处理（A）

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

分析证书(COA)

输入产品批号来搜索 分析证书(COA) 。批号可以在产品标签上"批“ （Lot或Batch）字后找到。

已有该产品？

在文件库中查找您最近购买产品的文档。

访问文档库

Jiawen Yong et al.
International journal of molecular sciences, 23(15) (2022-08-13)
Ciliary neurotrophic factor (CNTF) was identified as a survival factor in various types of peripheral and central neurons, glia and non-neural cells. At present, there is no available data on the expression and localization of CNTF-receptors in cementoblasts as well
Jiawen Yong et al.
Journal of cellular and molecular medicine, 25(20), 9710-9723 (2021-09-16)
Hypoxia-induced apoptosis of cementoblasts (OCCM-30) may be harmful to orthodontic treatment. Hypoxia-inducible factor 1-alpha (HIF-1α) mediates the biological effects during hypoxia. Little is known about the survival mechanism capable to counteract cementoblast apoptosis. We aimed to investigate the potential roles
Zahra S Thirouin et al.
The Journal of biological chemistry, 298(5), 101840-101840 (2022-03-22)
Posttranslational addition of a small ubiquitin-like modifier (SUMO) moiety (SUMOylation) has been implicated in pathologies such as brain ischemia, diabetic peripheral neuropathy, and neurodegeneration. However, nuclear enrichment of SUMO pathway proteins has made it difficult to ascertain how ion channels
Thomas Lanzicher et al.
Frontiers in physiology, 11, 173-173 (2020-04-08)
Titin is a large filamentous protein that forms a sarcomeric myofilament with a molecular spring region that develops force in stretched sarcomeres. The molecular spring has a complex make-up that includes the N2A element. This element largely consists of a
Yen-You Lin et al.
Journal of cellular physiology, 236(10), 6988-7000 (2021-03-28)
The pro-inflammatory cytokine interleukin 1 beta (IL-1β) plays a critical role in osteoarthritis (OA) disease pathogenesis. MicroRNA (miRNA) activity is related to inflammation in OA and some miRNAs specifically regulate IL-mediated degradation of cartilage type II collagen. Previous studies have
查看所有相关文献

相关内容

Human Kinome & InhibitorSelect™ Libraries

Human Kinome Poster: The InhibitorSelect™ Protein Kinase Inhibitor Libraries provide broad coverage of the human kinome as shown here. The depicted human kinome dendrogram of 518 kinases are classified into five broad groups, 90 families, and 145 subfamilies. Inhibitor coverage was assigned based upon published data related to potency (IC50, EC50, Kd, etc.) for individual kinases harvested from the literature. Colored dots denote which library contains an inhibitor with demonstrated potent activity against the designated kinase and do not necessarily reflect known specificity of the inhibitor. Coverage of lipid and atypical kinases are depicted as a separate dendrogram. As shown, Calbiochem® Protein Kinase Inhibitor Libraries cover all major kinase families including TK, CMGC, CAMK, AGC, CK1, STE, TKL, as well as Lipid or Atypical kinase families.

CARTA DE USO GENERAL 2016

()

PRODUCTO REGULADO POR LA SECRETARÍA DE SALUD

我们的科学家团队拥有各种研究领域经验，包括生命科学、材料科学、化学合成、色谱、分析及许多其他领域.

联系客户支持