C0993

CGP 57380

Name: CGP 57380
Brand: SIGMA
Price: 241.4 USD
Availability: InStock

≥98% (HPLC)

Synonym(s):

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

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5 MG

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About This Item

Empirical Formula (Hill Notation):

C₁₁H₉FN₆

CAS Number:

522629-08-9

Molecular Weight:

244.23

NACRES:

NA.77

PubChem Substance ID:

24724432

UNSPSC Code:

12352200

MDL number:

MFCD03861062

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

Key Documents

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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

Related Categories

Bioactive Small Molecule Inhibitors

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Show Differences

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This Item	P0040	SML2904	P0042
Sigma-Aldrich C0993 CGP 57380	Sigma-Aldrich P0040 PP1	Sigma-Aldrich SML2904 AGF347	Sigma-Aldrich P0042 PP2
assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)	assay ≥98% (HPLC)
form powder	form powder	form powder	form powder
Quality Level 100	Quality Level 100	Quality Level 100	Quality Level 100
storage temp. 2-8°C	storage temp. room temp	storage temp. 2-8°C	storage temp. 2-8°C
solubility DMSO: 10 mg/mL, clear, H₂O: <2 mg/mL	solubility DMSO: >20 mg/mL	solubility DMSO: 2 mg/L, clear	solubility DMSO: >10 mg/mL
color white to beige	color white to off-white	color white to beige	color white to off-white

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[1]
as an MNK1 inhibitor to block eIF4 complex to evaluate the contribution of interferon (IFN-γ) translation during m157- transgenic (Tg) stimulation[2]
as a β-catenin nuclear translocation inhibitor to analyze its effects on cytoplasmic and nuclear fractions of cells[3]

Biochem/physiol Actions

CGP 57380 is a β-catenin nuclear translocation inhibitor,[3] 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).[4]

CGP 57380 is a cell-permeable selective inhibitor of mitogen-activated protein kinase-interacting kinase 1 (MNK1).

Storage Class

11 - Combustible Solids

wgk

WGK 3

ppe

Eyeshields, Gloves, type N95 (US)

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Certificates of Analysis (COA)

Lot/Batch Number

0000406911

0000199789

0000069311

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Inflammatory signaling compromises cell responses to interferon alpha.

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

4E-BP restrains eIF4E phosphorylation.

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

Adenovirus-induced extracellular signal-regulated kinase phosphorylation during the late phase of infection enhances viral protein levels and virus progeny.

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

Monosodium urate crystal-induced pro-interleukin-1β production is post-transcriptionally regulated via the p38 signaling pathway in human monocytes.

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

FLI1 promotes protein translation via the transcriptional regulation of MKNK1 expression.

Chunlin Wang et al.

International journal of oncology, 56(2), 430-438 (2020-01-03)

The disruption of protein translation machinery is a common feature of cancer initiation and progression, and drugs that target protein translation offer new avenues for therapy. The translation initiation factor, eukaryotic initiation factor 4E (eIF4E), is induced in a number

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Global Trade Item Number

SKU	GTIN
C0993-5MG	04061832445229
C0993-25MG	04061832445212

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CGP 57380