CGP 57380

SKU: orb1300766

Description

CGP 57380 is a selective MNK1 inhibitor (IC50 = 2.2 μM) with minimal activity against related kinases like p38, JNK, ERK, PKC, and c-Src. It is a valuable research tool for studying MNK1's role in mRNA translation and oncogenesis in both cellular and animal models of cancer and inflammation.

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 522629-08-9
• MW: 244.23
• Purity: 99.89% (May vary between batches)
• Formula: C₁₁H₉FN₆
• SMILES: Nc1ncnc2[nH]nc(Nc3ccc(F)cc3)c12
• Target: MNK|||Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (8.19 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:45 mg/mL (184.25 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  MNK1:2.2 μM
• In Vivo:
  CGP57380 (40 mg/kg/d i.p.) potently abrogates the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs.
• In Vitro:
  CGP57380 inhibits phosphorylation of eIF4E in vitro with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). CGP57380 prevents the serial replating function of BC progenitors.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Apoptosis, CGP 57380, CGP57380, CGP-57380, MAPK interacting kinase, MAP kinase interacting kinase, Inhibitor, Mitogen activated protein kinase interacting kinase, MNK, MNK1, MNK1 Inhibitor, MNK2, inhibit

Compound Identifiers

PubChem CID

11644425