Catalog Number: 4931
Chemical Name: N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine
Biological Activity
Neuropilin 1 (NRP1) receptor antagonist; inhibits VEGFA binding to the NRP1 b1 domain. Has no effect on VEGFA binding to VEGFR-1 and VEGFR-2. Reduces VEGFA-induced VEGFR-2 tyrosine phosphorylation in HUVECs. Also attenuates VEGFA-induced HUVEC cell migration and reduces A549 lung carcinoma cell viability in vitro. Increases chemo-sensitivity of A549 cells in combination with Taxol (Cat. No. 1097). Blocks pro-tumorigenic M2 polarization in glioma-associated microglia and macrophages and reduces tumor growth and vascularization in NSG mice.
Technical Data
  • M.Wt:
    497.57
  • Formula:
    C17H19N7O5S3
  • Solubility:
    Soluble to 100 mM in 1eq. NaOH and to 100 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    1018927-63-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction.
    Jarvis et al.
    J.Med.Chem., 2010;53:2215
  2. Ablation of Neuropilin 1 from glioma-associated microglia and macrophages slows tumor progression.
    Miyauchi et al.
    Oncotarget, 2016;7:9801
  3. VEGF-A acts via neuropilin-1 to enhance epidermal cancer stem cell survival and formation of aggressive and highly vascularized tumors.
    Grun et al.
    Oncogene., 2016;35:4379
Citations:

The citations listed below are publications that use Tocris products. Selected citations for EG 00229 include:

1 Citations: Showing 1 - 1

  1. Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway.
    Authors: Nissen Et al.
    J.Neurochem. 2013;127:394

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