CGP 57380 - ≥98%, high purity , CAS No.522629-08-9, Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2

Item Number

C274776

• Synonyms: NSC 741567 | SR-02000000869 | A902707 | BISBENTIAMINE [MI] | NCIOpen2_009023 | SCHEMBL16714452 | NCGC00162380-01 | HMS3648M14 | C75450 | HMS3653G22 | Q27087429 | AKOS024457265 | SDCCGSBI-0086774.P002 | HMS3677D16 | NCGC00162380-02 | HMS3673K05 | BDBM50298
• Specifications & Purity: Moligand™, ≥98%
• 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 -20°C
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of MAPK interacting serine/threonine kinase 1;Inhibitor of MAPK interacting serine/threonine kinase 2
• Note: Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Product Description

Store at +4°C. The product can be stored for up to 12 months.

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).