CGP 57380A selective inhibitor of MNK1

CGP 57380 (CAS 522629-08-9)

CGP 57380 | CAS 522629-08-9 is rated 5.0 out of 5 by 1.
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Synonym: MNK1 Inhibitor
Application: A selective inhibitor of MNK1
CAS Number: 522629-08-9
Purity: >98%
Molecular Weight: 244.23
Molecular Formula: C11H9FN6
* Refer to Certificate of Analysis for lot specific data (including water content).
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CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 (mitogen-activated protein kinase-interacting kinase 1; MNK1; IC50 = 2.2 μM) with no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases. CGP 57380 effectively inhibits eIF4E phosphorylation (IC50 = 3 μM) by MNK1 in 293 human embryonic kidney cells and serves as a useful tool in studying Mnk1-mediated cellular signaling. CGP 57380 is an inhibitor of ARK-2, BRSK2, ChoK, Dyrk3, Lck, Mnk2 and SGK.


References

1. Knauf, U., et al. 2001. Mol. Cell. Biol. 21: 5500-5511. PMID: 11463832
2. Morley, S.J., et al. 2002. J. Biol. Chem. 277: 32855-32859. PMID: 12138083
3. Topisirovic, I., et al. 2004. Cancer Res. 64: 8639-8642. PMID: 15574771
4. Walsh, D., et al. 2004. Genes Dev. 18: 660-672. PMID: 15075293
5. Worch, J., et al. 2004. Oncogene. 23: 9162-9172. PMID: 15516979

Physical State :
Solid
Solubility :
Soluble in DMSO (~ 30 mg/ml), water (< 2 mg/ml), ethanol (~ 0.25 mg/ml), DMF (~ 30 mg/ml), and 1:1 solution of DMSO:PBS (pH 7.2) (~ 0.5 mg/ml).
Storage :
Store at 4° C
Melting Point :
190.15° C (Predicted)
Boiling Point :
~541.64° C at 760 mmHg (Predicted)
Density :
~1.59 g/cm3 (Predicted)
Refractive Index :
n20D 1.81 (Predicted)
IC50 :
Mnk1: IC50 = 0.87 µM (human); Mnk2: IC50 = 1.6 µM (human); SGK: IC50 = 2.7 µM (human); Phosphorylation of eIF4E in response to TNF-α, arsenite, anisomycin, PMA, or fetal calf serum in 293 cells: IC50 = 3 µM; PKR: IC50 = 5 µM (human)
pK Values :
pKa: 11.25 (Predicted), pKb: 5.16 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
11644425
MDL Number :
MFCD03861062
SMILES :
C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F

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Certificate of Analysis

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CGP 57380  Product Citations

See how others have used CGP 57380. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 26609108  Kumar, K. et al. 2016. Mol. Cancer Res. 14: 216-27.

PMID: # 25193863  Eckerdt, F. et al. 2014. Oncotarget. 5: 8442-8451.

PMID: # 17130135  Chrestensen, C.A. et al. 2007. J. Biol. Chem. 282: 4243-4252.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Eckerdt Eckerdt, F. et al. (PubMed 25193863) used product sc-202993 (CGP 57380), a Mnk 1/2 inhibitor, to determine its effect on mTORC1 sensitization to rapamycin in medulloblastoma cells. Found that CGP 57380 prevented activation of eIF4E, sensitizing mTORC1 and significantly increasing rapamycin efficacy towards medulloblastoma cells. -SCBT Publication Review
Date published: 2015-07-15
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