CGP 57380

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC50 of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

Product Specifications

CAS Number

[522629-08-9]

UNSPSC

12352005

Hazard Statement

H319

Target

Apoptosis; MNK

Type

Reference compound

Related Pathways

Apoptosis; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/CGP-57380.html

Purity

98.71

Solubility

DMSO : ≥ 100 mg/mL|H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

NC1=NC=NC2=C1C(NC3=CC=C(F)C=C3)N=N2

Molecular Formula

C11H9FN6

Molecular Weight

244.23

Precautions

H319

References & Citations

[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