Cell Sheet Migration Inhibitor, Locostatin An inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction

Cell Sheet Migration Inhibitor, Locostatin (CAS 133812-16-5)

Cell Sheet Migration Inhibitor, Locostatin | CAS 133812-16-5 is rated 5.0 out of 5 by 1.
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Application: An inhibitor of Raf kinase inhibitor protein (RKIP)/Raf1 kinase interaction
CAS Number: 133812-16-5
Purity: ≥98%
Molecular Weight: 245.3
Molecular Formula: C14H15NO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cell Sheet Migration Inhibitor, Locostatin is a cell-permeable N-(crotonyl)oxazolidinone compound that acts as a potent inhibitor of RKIP (Raf kinase inhibitor protein)/Raf-1 kinase interaction. Cell Sheet Migration Inhibitor, Locostatin has been shown to block eukaryotic cell migration (IC50 = 14 μM for inhibition of wound closure in MDCK cell monolayers) and decrease formation of lamellipodial protrusions at the wound margin. Cell Sheet Migration Inhibitor, Locostatin also inhibits early development in frog embryos and tissue dynamics in embryonic explants. Displays no antibacterial activity. May serve as a useful tool for studying RKIP-mediated signaling pathways. Although locostatin is an irreversible inhibitor of RKIP, its cellular effects are generally reversible due to new biosynthesis.


References

Bement, W.M., et al. 2005. Chem. Biol. 12, 953. Zhu, S., et al. 2005. Chem. Biol. 12, 981. Mc Henry, K.T., et al. 2002. Chembiochem 3, 1105.

Physical State :
Solid
Solubility :
Soluble in methanol (50 mg/ml), and DMSO (5 mg/ml).
Storage :
Store at 4° C
Melting Point :
84-88° C (lit.)
Boiling Point :
351.04° C at 760 mmHg (Predicted)
Density :
1.21 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
Optical Activity :
α20/D +76°°, c = 1 in chloroform
IC50 :
eukaryotic cell migration: IC50 = 14 µM (MDCK cell monolayers)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
5702600
MDL Number :
MFCD00278769
SMILES :
CC=CC(=O)N1C(COC1=O)CC2=CC=CC=C2

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Certificate of Analysis

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Cell Sheet Migration Inhibitor, Locostatin  Product Citations

See how others have used Cell Sheet Migration Inhibitor, Locostatin. Click on the entry to view the PubMed entry .

Citations 1 to 3 of 3 total

PMID: # 17668446  Mc Henry, KT. et al. 2008. J. Cell. Biochem. 103: 972-985.

Tweeten, KA et al. 2008. BIOS. 79: 183-190.

PMID: # 16183022  Zhu, S. et al. 2005. Chem. Biol. 12: 981-991.

Citations 1 to 3 of 3 total
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Rated 5 out of 5 by from Zhu Zhu, S. et al. (PubMed 16183022) determined locostatin selectively targets RKIP and interrupts its ability to interact with Raf1. This interaction between locostatin and RKIP significantly reduced cell migration rate. -SCBT Publication Review
Date published: 2015-03-04
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