CGP 57380 CAS: 522629-08-9
MF: C11H9FN6
MW: 244.23
A selective inhibitor of MNK1.

CGP 57380 (CAS 522629-08-9)

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Alternate Names: MNK1 Inhibitor
Application CGP 57380 is a selective inhibitor of MNK1
CAS 등록번호: 522629-08-9
순도: >98%
분자량: 244.23
분자식: C11H9FN6
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
* 참조분석증명서대량의 측정 데이터(함수량포함).

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
용해도 :
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).
저장 :
Store at 4° C
녹는점 :
190.15° C (Predicted)
비등점 :
~541.64° C at 760 mmHg (Predicted)
밀도 :
~1.59 g/cm3 (Predicted)
굴절률 :
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)
연구용으로만 사용가능합니다. 진단이나 치료용으로 사용불가합니다.
WGK Germany :
3
PubChem CID :
MDL Number :
MFCD03861062
SMILES :
C1=CC(=CC=C1NC2=C3C(=NC=NC3=NN2)N)F

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CGP 57380 (CAS 522629-08-9)  논문정보

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PMID: # 30842251  Eckerdt, F.|Bell, JB.|Beauchamp, EM.|Clymer, J.|Blyth, GT.|Kosciuczuk, EM.|Ma, Q.|Chen, DZ.|Horbinski, C.|Goldman, S.|Munshi, HG.|Hashizume, R.|Platanias, LC.| et al. 2019. Mol Cancer Res. 17: 1305-1315.

PMID: # 29042487  Bell, JB.|Eckerdt, F.|Dhruv, HD.|Finlay, D.|Peng, S.|Kim, S.|Kroczynska, B.|Beauchamp, EM.|Alley, K.|Clymer, J.|Goldman, S.|Cheng, SY.|James, CD.|Nakano, I.|Horbinski, C.|Mazar, AP.|Vuori, K.|Kumthekar, P.|Raizer, J.|Berens, ME.|Platanias, LC.| et al. 2018. Mol Cancer Res. 16: 32-46.

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.

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