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Submit ReviewCGP 57380
说明： Selective inhibitor of Mnk1
化学名： N3-(4-Fluorophenyl)-1H-pyrazolo-[3,4-d]pyrimidine-3,4-diamine
纯度： ≥98% (HPLC)
生物活性 for CGP 57380
CGP 57380 is an inhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) (IC50 = 2.2 μM) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases. Blocks phosphorylation of eIF4E in cellular assays (IC50 = 3 μM) and inhibits LPS-induced TNFα expression in macrophages.
化合物库 for CGP 57380
CGP 57380 is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
技术数据 for CGP 57380
| 分子量 | 244.23 |
| 公式 | C11H9FN6 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 522629-08-9 |
| PubChem ID | 11644425 |
| InChI Key | UQPMANVRZYYQMD-UHFFFAOYSA-N |
| Smiles | NC1=C2C(NC3=CC=C(F)C=C3)=NNC2=NC=N1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for CGP 57380
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 24.42 | 100 |
制备储备液 for CGP 57380
以下数据基于产品分子量 244.23。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.09 mL | 20.47 mL | 40.95 mL |
| 5 mM | 0.82 mL | 4.09 mL | 8.19 mL |
| 10 mM | 0.41 mL | 2.05 mL | 4.09 mL |
| 50 mM | 0.08 mL | 0.41 mL | 0.82 mL |
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产品说明书 for CGP 57380
参考文献 for CGP 57380
参考文献是支持产品生物活性的出版物。
Knauf et al (2001) Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol.Cell.Biol. 21 5500 PMID: 11463832
Ishida et al (2003) Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ.Res. 93 1218 PMID: 14605021
Andersson and Sundler (2006) Posttranscriptional regulation of TNFα expression via eukaryotic initiation factor 4E (eIF4E) phosphorylation in mouse macrophages. Cytokine 33 52 PMID: 16431125
If you know of a relevant reference for CGP 57380, please let us know.
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关键词: CGP 57380, CGP 57380 supplier, Selective, inhibitors, inhibits, Mnk1, Kinases, CGP57380, Mnk, 2731, Tocris Bioscience
7 篇 CGP 57380 的引用文献
引用文献是使用了 Tocris 产品的出版物。 CGP 57380 的部分引用包括：
Brown and Gromeier (2017) MNK Controls mTORC1:Substrate Association through Regulation of TELO2 Binding with mTORC1. Cell Rep 18 1444 PMID: 28178522
Origanti et al (2012) Ornithine decarboxylase mRNA is stabilized in an mTORC1-dependent manner in Ras-transformed cells. Biochem J 442 199 PMID: 22070140
Riz et al (2016) Noncanonical SQSTM1/p62-Nrf2 pathway activation mediates proteasome inhibitor resistance in multiple myeloma cells via redox, metabolic and translational reprogramming. Oncotarget 7 66360 PMID: 27626179
Dumoulin et al (2013) Extracellular Signal-Regulated Kinase (ERK) Activity During Sleep Consolidates Cortical Plasticity In Vivo. Cereb Cortex PMID: 24047601
Royall et al (2015) Murine norovirus 1 (MNV1) replication induces translational control of the host by regulating eIF4E activity during infection. Neurochem Res 290 4748 PMID: 25561727
Brown et al (2014) Mitogen-activated protein kinase-interacting kinase regulates mTOR/AKT signaling and controls the serine/arginine-rich protein kinase-responsive type 1 internal ribosome entry site-mediated translation and viral oncolysis. J Biol Chem 88 13149 PMID: 25187540
Melemedjian et al (2010) IL-6- and NGF-induced rapid control of protein synthesis and nociceptive plasticity via convergent signaling to the eIF4F complex. J Neurosci 30 15113 PMID: 21068317
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CGP 57380 的评论
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(CGP57380, 10 μM).
By
Anonymous on 12/11/2019
分析类型： In Vitro
种属： Human
细胞系/组织： LP-1 cell line
Cells were treated with MG-132 (15 µM) for 18 hours in the absence or presence of an eIF4E/eIF4G interaction inhibitor (4EGI-1, 50 µM) or an MNK inhibitor (CGP57380, 10 μM).
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.