product name CGP 57380
Description: CGP 57380 is a potent and selcetive MNK1 inhibitor with IC50 of 2.2 μM, it exhibited no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. In 293 cells, CGP 57380 (10 μM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 μM. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way.
References: Mol Cell Biol. 2001;21:5500-11; Circ Res. 2003;93:1218-24; Proc Natl Acad Sci U S A. 2013;110:E2298-307.
244.23
Formula
C11H9FN6
CAS No.
522629-08-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 48 mg/mL (196.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
4% DMSO+30% PEG 300+ddH2O: 10 mg/mL
Synonyms
other peoduct :
| In Vitro |
In vitro activity: CGP57380 inhibits phosphorylation of eIF4E in cellular assays 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. Kinase Assay: CGP 57380 is potent inhibitor of MNK1 with IC50 value of 2.2 μM. Cell Assay: In 293 cells, CGP 57380 (10 μM) inhibited eIF4E phosphorylation in response to fetal calf serum (FCS), arsenite, anisomycin, PMA or tumor necrosis factor alpha. Also, CGP 57380 increased the cap-dependent reporter rluc. In cellular assays, CGP 57380 inhibited eIF4E phosphorylation with IC50 value of 3 μM. In rat vascular smooth muscle cells, CGP 57380 inhibited eIF4E phosphorylation, protein synthesis and VSMC hypertrophy induced by angiotensin II in a dose dependent way. In mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. In bone marrow-derived macrophages, CGP 57380 significantly inhibited the production of proinflammatory cytokines monocyte chemoattractant protein-1, TNF and IL-6. |
|---|---|
| In Vivo | CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs. |
| Animal model | In mouse macrophages, CGP 57380 concentration-dependently inhibited TNFα production stimulated by Escherichia coli lipopolysaccharide (LPS) through posttranscriptional regulation. Also, CGP 57380 inhibited eIF4E phosphorylation. |
| Formulation & Dosage | |
| References | Mol Cell Biol. 2001 Aug;21(16):5500-11; Circ Res. 2003 Dec 12;93(12):1218-24; Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307. |
