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Key Documents

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C0993

Sigma-Aldrich

CGP 57380

≥98% (HPLC)

Sinónimos:

CGP57380, N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine

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About This Item

Fórmula empírica (notación de Hill):
C11H9FN6
Número de CAS:
522629-08-9
Peso molecular:
244.23
MDL number:
MFCD03861062
UNSPSC Code:
12352200
PubChem Substance ID:
24724432
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 10 mg/mL, clear
H2O: <2 mg/mL

storage temp.

2-8°C

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)

InChI key

UQPMANVRZYYQMD-UHFFFAOYSA-N

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).

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

ppe

Eyeshields, Gloves, type N95 (US)

Certificados de análisis (COA)

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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
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
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
Jean Chemin et al.
Scientific reports, 9(1), 15642-15642 (2019-11-02)
Cav3 / T-type Ca2+ channels are dynamically regulated by intracellular Ca2+ ions, which inhibit Cav3 availability. Here, we demonstrate that this inhibition becomes irreversible in the presence of non-hydrolysable ATP analogs, resulting in a strong hyperpolarizing shift in the steady-state
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
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