Molecular structure of CGP 57380, CAS Number: 522629-08-9
CGP 57380 (CAS 522629-08-9)
See product citations (6)
Alternate Names:
MNK1 Inhibitor
Application:
CGP 57380 is a selective inhibitor of MNK1
CAS Number:
522629-08-9
Purity:
>98%
Molecular Weight:
244.23
Molecular Formula:
C11H9FN6
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of mitogen-activated protein kinase-interacting kinase 1 (MNK1; IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases. CGP 57380 effectively inhibits eIF4E phosphorylation (IC50 = 3 µM) by MNK1 in 293 human embryonic kidney cells and serves as a useful tool in studying MNK1-mediated cellular signaling.
CGP 57380 (CAS 522629-08-9) References
- Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. | Knauf, U., et al. 2001. Mol Cell Biol. 21: 5500-11. PMID: 11463832
- Phosphorylation of eukaryotic initiation factor (eIF) 4E is not required for de novo protein synthesis following recovery from hypertonic stress in human kidney cells. | Morley, SJ. and Naegele, S. 2002. J Biol Chem. 277: 32855-9. PMID: 12138083
- Phosphorylation of initiation factor 4E is resistant to SB203580 in cells expressing a drug-resistant mutant of stress-activated protein kinase 2a/p38. | Morley, SJ. and Naegele, S. 2003. Cell Signal. 15: 741-9. PMID: 12781867
- Phosphorylation of eIF4E by Mnk-1 enhances HSV-1 translation and replication in quiescent cells. | Walsh, D. and Mohr, I. 2004. Genes Dev. 18: 660-72. PMID: 15075293
- The serine-threonine kinase MNK1 is post-translationally stabilized by PML-RARalpha and regulates differentiation of hematopoietic cells. | Worch, J., et al. 2004. Oncogene. 23: 9162-72. PMID: 15516979
- Phosphorylation of the eukaryotic translation initiation factor eIF4E contributes to its transformation and mRNA transport activities. | Topisirovic, I., et al. 2004. Cancer Res. 64: 8639-42. PMID: 15574771
- Shiga toxins activate translational regulation pathways in intestinal epithelial cells. | Colpoys, WE., et al. 2005. Cell Signal. 17: 891-9. PMID: 15763431
- MNK1 expression increases during cellular senescence and modulates the subcellular localization of hnRNP A1. | Ziaei, S., et al. 2012. Exp Cell Res. 318: 500-8. PMID: 22227431
- MNK1 inhibitor CGP57380 overcomes mTOR inhibitor-induced activation of eIF4E: the mechanism of synergic killing of human T-ALL cells. | Huang, XB., et al. 2018. Acta Pharmacol Sin. 39: 1894-1901. PMID: 30297804
- Rare germline variants in the E-cadherin gene CDH1 are associated with the risk of brain tumors of neuroepithelial and epithelial origin. | Förster, A., et al. 2021. Acta Neuropathol. 142: 191-210. PMID: 33929593
Inhibitor of:
4E-BP2, ARK-2, BRSK2, c-Myb, ChoK, DNA-PKCS, Dyrk3, eIF4E, eIF4G, Elk-1, GNGT2, Lck, Mnk1, Mnk2, MOB3A, MSK1, MSK2, PC-PLD2, Protease, Ribosomal Protein L11, S-100A5, SEC14L5, SGK, and UHMK1.Activator of:
AF-10, EG435337, eIF4B, MYCBP, Myocardin, Nix, Rad21, and Shank 2.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
CGP 57380, 5 mg | sc-202993 | 5 mg | $172.00 |