1210945-69-9 Usage
Uses
EG 00229 Trifluoroacetic Acid Salt is an antagonist of the VEGFA receptor neuropilin (NRP1). This antagonism can result in the attenuation of prostate carcinoma cell proliferation.
Biological Activity
eg00229 is a small molecule inhibitor of neuropilin-1(nrp1) with an ic50 of 3μm [1].eg00229 has been reported to inhibit vegf-a binding to pae/nrp1 in the nrp1and bt-vegf-a binding to purified nrp1 b1 domain in a cell-free assay with an ic50 value of 8μm and 3μm, respectively. in addition, eg00229 has also shown the inhibition of vegf-a binding to vegfr2, vegfr1 and nrp1 in human umbilical vein endothelial cells (huvecs) in a dose-dependent manner with an ic50 value of 23μm [1]. besides, eg00229 has been revealed to prevent tuftsin binding to the nrp1 which is at the cell surface. moreover, eg00229 has been noted to suppress the anti-inflammatory m2 shift in microglia induced by tuftsin and thus potently prevent tuftsin’s action [2].
references
[1] jarvis a1, allerston ck, jia h, herzog b, garza-garcia a, winfield n, ellard k, aqil r, lynch r, chapman c, hartzoulakis b, nally j, stewart m, cheng l, menon m, tickner m, djordjevic s, driscoll pc, zachary i, selwood dl.small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor a (vegf-a) interaction. j med chem. 2010 mar 11;53(5):2215-26. [2] nissen jc1, selwood dl, tsirka se. tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. j neurochem. 2013 nov;127(3):394-402.
Check Digit Verification of cas no
The CAS Registry Mumber 1210945-69-9 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,1,0,9,4 and 5 respectively; the second part has 2 digits, 6 and 9 respectively.
Calculate Digit Verification of CAS Registry Number 1210945-69:
(9*1)+(8*2)+(7*1)+(6*0)+(5*9)+(4*4)+(3*5)+(2*6)+(1*9)=129
129 % 10 = 9
So 1210945-69-9 is a valid CAS Registry Number.
1210945-69-9Relevant articles and documents
Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction
Jarvis, Ashley,Allerston, Charles K.,Jia, Haiyan,Herzog, Birger,Garza-Garcia, Acely,Winfield, Natalie,Ellard, Katie,Aqil, Rehan,Lynch, Rosemary,Chapman, Chris,Hartzoulakis, Basil,Nally, James,Stewart, Mark,Cheng, Lili,Menon, Malini,Tickner, Michelle,Djordjevic, Snezana,Driscoll, Paul C.,Zachary, Ian,Selwood, David L.
experimental part, p. 2215 - 2226 (2010/08/21)
We report the molecular design and synthesis of EG00229,2, the first small molecule ligand for the VEGF-A receptor neuropilin 1 (NRPl) and the structural characterization of NRPl-ligand complexes by NMR spectroscopy and X-ray crystallography. Mutagenesis studies localized VEGF-A binding in the NRPl bl domain and a peptide fragment of VEGF-A was shown to bind at the same site by NMR, providing the basis for small molecule design. Compound 2 demonstrated inhibition of VEGF-A binding to NRPl and attenuated VEGFR2 phosphorylation in endothelial cells. Inhibition of migration of endothelial cells was also observed. The viability of A549 lung carcinoma cells was reduced by 2, and it increased the potency of the cytotoxic agents paclitaxel and 5-fluorouracil when given in combination. These studies provide the basis for design of specific small molecule inhibitors of ligand binding to NRP1.
