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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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C424479-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $172.90 |
MNK inhibitor
Synonyms | CGP 57380 | 522629-08-9 | CGP-57380 | MNK1 Inhibitor | N3-(4-fluorophenyl)-1h-pyrazolo[3,4-d]pyrimidine-3,4-diamine | 3-N-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine | CHEMBL1240885 | CGP57380 | SCHEMBL987991 | GTPL6010 | SCHEMBL16714452 | CHEBI:92749 | DTXSID50469 |
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Specifications & Purity | Moligand™, 10mM in DMSO |
Biochemical and Physiological Mechanisms | Low-molecular-weight kinase inhibitor of MAP-kinase interacting kinase-1 (MNK1) and MNK2 (IC 50 values are 0.87 and 1.6 μM, respectively). Inhibits a range of other kinases (IC 50 values in μM shown in brackets) including: CKI (0.51) Aurora B (2.5) DYRK3 |
Storage Temp | Store at -80°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Product Description | 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. Biochemical mechanism: 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). |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 3-N-(4-fluorophenyl)-2H-pyrazolo[3,4-d]pyrimidine-3,4-diamine |
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INCHI | 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 |
Canonical SMILES | C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F |
Isomeric SMILES | C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F |
PubChem CID | 11644425 |
Molecular Weight | 244.23 |
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Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H319:Causes serious eye irritation |
Precautionary Statements | P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P337+P317:If eye irritation persists: Get medical help. |