CGP 57380

• CAT Number: I013945
• CAS Number: 522629-08-9
• Molecular Formula: C₁₁H₉FN₆
• Molecular Weight: 244.23
• Purity: ≥95%
• Target: MNK
• Solubility: DMSO: ≥ 43 mg/mL
• IUPAC Name: 3-N-(4-fluorophenyl)-3H-pyrazolo[3,4-d]pyrimidine-3,4-diamine
• 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/h1-5,11,16H,(H2,13,14,15)
• InChIKey: SIIPGZWXUQVYMG-UHFFFAOYSA-N
• SMILES: C1=CC(=CC=C1NC2C3=C(N=CN=C3N)N=N2)F

CGP57380 (Cat. No: I013945) is a potent MNK1 inhibitor with an IC50 of 2.2 μM and shows no inhibitory activity against p38, JNK1, ERK1 and-2, PKC, or Chemicalbookc-Src-like kinases. In addition, CGP57380 can up-regulate β-catenin and enhance radiation-induced apoptosis.

Reference

[1]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11.[2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6.[3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40.[4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307.