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CGP 57380

Catalog No. T6440   CAS 522629-08-9
Synonyms: MNK1 Inhibitor

CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.

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CGP 57380 Chemical Structure
CGP 57380, CAS 522629-08-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 39.00
2 mg In stock $ 56.00
5 mg In stock $ 92.00
10 mg In stock $ 145.00
25 mg In stock $ 275.00
50 mg In stock $ 458.00
100 mg In stock $ 659.00
200 mg In stock $ 923.00
1 mL * 10 mM (in DMSO) In stock $ 115.00
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Purity: 99.89%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases.
Targets&IC50 MNK1:2.2 μM
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. [1] CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] CGP57380 prevents the serial replating function of BC progenitors. [4]
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. [4]
Kinase Assay Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors.
Synonyms MNK1 Inhibitor
Molecular Weight 244.23
Formula C11H9FN6
CAS No. 522629-08-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: <1 mg/mL

Ethanol: <1 mg/mL

DMSO: 45 mg/mL (184.3 mM)

TargetMolReferences and Literature

1. Knauf U, et al. Mol Cell Biol. 2001, (16), 5500-5511. 2. Ishida M, et al. Circ Res. 2003, 93(12), 1218-1224. 3. Chrestensen CA, et al. Genes Cells. 2007, 12(10), 1133-1140. 4. Lim S, et al. Proc Natl Acad Sci U S A. 2013, 110(25), E2298-E2307.

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Reprogramming Compound Library Inhibitor Library Bioactive Lipid Compound Library NO PAINS Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max Bioactive Compound Library Anti-Cancer Compound Library Anti-Liver Cancer Compound Library

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Keywords

CGP 57380 522629-08-9 Apoptosis MAPK MNK Mitogen activated protein kinase interacting kinase Inhibitor MAPK interacting kinase inhibit CGP57380 MNK1 Inhibitor MAP kinase interacting kinase CGP-57380 inhibitor

 

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