Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 45 mg/mL (184.3 mM)
You can also refer to dose conversion for different animals. More
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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