C0993
CGP 57380
≥98% (HPLC)
别名:
CGP57380, N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine
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关于此项目
经验公式（希尔记法）:
C11H9FN6
化学文摘社编号:
分子量:
244.23
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
CGP 57380, ≥98% (HPLC)
InChI key
UQPMANVRZYYQMD-UHFFFAOYSA-N
SMILES string
Nc1ncnc2[nH]nc(Nc3ccc(F)cc3)c12
InChI
1S/C11H9FN6/c12-6-1-3-7(4-2-6)16-11-8-9(13)14-5-15-10(8)17-18-11/h1-5H,(H4,13,14,15,16,17,18)
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 10 mg/mL, clear
H2O: <2 mg/mL
storage temp.
2-8°C
Quality Level
相关类别
Application
CGP 57380 has been used:
- as a mitogen-activated protein kinase-interacting kinase 1 (MNK1) inhibitor to investigate the role of Mnk1 on eukaryotic translation initiation factor 4F (eIF4F) assembly and Newcastle disease virus (NDV) replication in HeLa cells
- as an MNK1 inhibitor to block eIF4 complex to evaluate the contribution of interferon (IFN-γ) translation during m157- transgenic (Tg) stimulation
- as a β-catenin nuclear translocation inhibitor to analyze its effects on cytoplasmic and nuclear fractions of cells
Biochem/physiol Actions
CGP 57380 is a β-catenin nuclear translocation inhibitor, which prevents the proliferation of several cancers. It enhances radiation-induced apoptosis in nasopharyngeal carcinoma (NPC). CGP 57380 upregulates β-catenin in the cytoplasm and inhibits epithelial-mesenchymal transition (EMT).
CGP 57380 is a cell-permeable selective inhibitor of mitogen-activated protein kinase-interacting kinase 1 (MNK1).
存储类别
11 - Combustible Solids
wgk
WGK 3
ppe
Eyeshields, Gloves, type N95 (US)
Yeon-Ho Chung et al.
Scientific reports, 6, 34533-34533 (2016-10-04)
IL-1β is a key mediator of sterile inflammation in response to endogenous particulates, a type of damage-associated molecular pattern (DAMPs) molecule derived from damaged cells. Despite the well-known role of sterile particulates such as monosodium urate (MSU) crystals as inflammasome
Michael Schümann et al.
Cancer research, 66(3), 1282-1288 (2006-02-03)
The Raf/mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase (MEK)/ERK signaling cascade enhances tumor cell proliferation in many cases. Here, we show that adenovirus type 5, a small DNA tumor virus used in experimental cancer therapy, strongly induces ERK phosphorylation during the
David Müller et al.
Translation (Austin, Tex.), 1(2), e25819-e25819 (2013-01-01)
In eukaryotes, mRNA translation is dependent on the cap-binding protein eIF4E. Through its simultaneous interaction with the mRNA cap structure and with the ribosome-associated eIF4G adaptor protein, eIF4E physically posits the ribosome at the 5' extremity of capped mRNA. eIF4E
W-C Huangfu et al.
Oncogene, 31(2), 161-172 (2011-06-15)
Interferon alpha (IFNα) is widely used for treatment of melanoma and certain other malignancies. This cytokine as well as the related IFNβ exerts potent anti-tumorigenic effects; however, their efficacy in patients is often suboptimal. Here, we report that inflammatory signaling
Krishan Kumar et al.
Molecular cancer research : MCR, 14(2), 216-227 (2015-11-27)
Human pancreatic ductal adenocarcinoma (PDAC) tumors are associated with dysregulation of mRNA translation. In this report, it is demonstrated that PDAC cells grown in collagen exhibit increased activation of the MAPK-interacting protein kinases (MNK) that mediate eIF4E phosphorylation. Pharmacologic and
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