522629-08-9 Usage
Description
CGP 57380 is a small molecule compound that serves as a potent inhibitor of mitogen-activated protein kinase-interacting kinase 1 (MNK1). It is characterized by its ability to interfere with the eukaryotic translation initiation factor 4F (eIF4F) assembly and has been widely utilized in various cellular and molecular biology research applications.
Uses
Used in Cellular and Molecular Biology Research:
CGP 57380 is used as an MNK1 inhibitor for investigating the role of Mnk1 on eIF4F assembly and its influence on cellular processes such as translation and gene expression. This application is crucial in understanding the underlying mechanisms of various cellular functions and responses to stimuli.
Used in Virology:
CGP 57380 is used as an MNK1 inhibitor to study the replication of Newcastle disease virus (NDV) in HeLa cells. By blocking the eIF4 complex, researchers can evaluate the contribution of interferon (IFN-γ) translation during m157-transgenic (Tg) stimulation, providing insights into the virus-host interactions and potential therapeutic targets.
Used in Signal Transduction Research:
CGP 57380 is used as a β-catenin nuclear translocation inhibitor to analyze its effects on the cytoplasmic and nuclear fractions of cells. This application aids in understanding the role of β-catenin in cellular signaling pathways and its involvement in various cellular processes, including cell proliferation, differentiation, and development.
Biological Activity
Inhibitor of MAP-kinase interacting kinase-1 (Mnk1, MKNK1) (IC 50 = 2.2 μ M) that displays selectivity over p38, JNK1, ERK1, ERK2, PKC and c-src family kinases. Blocks phosphorylation of eIF4E in cellular assays (IC 50 = 3 μ M) and inhibits LPS-induced TNF α expression in macrophages.
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).
references
[1]. knauf u, tschopp c, gram h. negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. mol cell biol, 2001, 21(16): 5500-5511.[2]. ishida m, ishida t, nakashima h, et al. mnk1 is required for angiotensin ii-induced protein synthesis in vascular smooth muscle cells. circ res, 2003, 93(12): 1218-1224. [3]. andersson k, sundler r. posttranscriptional regulation of tnfalpha expression via eukaryotic initiation factor 4e (eif4e) phosphorylation in mouse macrophages. cytokine, 2006, 33(1): 52-57.[4]. rowlett rm, chrestensen ca, nyce m, et al. mnk kinases regulate multiple tlr pathways and innate proinflammatory cytokines in macrophages. am j physiol gastrointest liver physiol, 2008, 294(2): g452-459.
Check Digit Verification of cas no
The CAS Registry Mumber 522629-08-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,2,2,6,2 and 9 respectively; the second part has 2 digits, 0 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 522629-08:
(8*5)+(7*2)+(6*2)+(5*6)+(4*2)+(3*9)+(2*0)+(1*8)=139
139 % 10 = 9
So 522629-08-9 is a valid CAS Registry Number.
InChI:InChI=1/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)
