EG 00229

Description: Neuropilin 1 (NRP1) receptor antagonist; inhibits VEGFA binding to NRP1
Chemical Name: N2-[[3-[(2,1,3-Benzothiadiazol-4-ylsulfonyl)amino]-2-thienyl]carbonyl]-L-arginine
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (3)
Pathways (1)

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.

Compound Libraries

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Technical Data

M. Wt 497.57
Formula C17H19N7O5S3
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1018927-63-3
PubChem ID 44631827
InChI Key ZWWMEDURALZMEV-NSHDSACASA-N
Smiles O=S(C1=CC=CC2=NSN=C12)(NC3=C(C(N[C@H](C(O)=O)CCCNC(N)=N)=O)SC=C3)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Product Datasheets

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References

References are publications that support the biological activity of the product.

Jarvis et al (2010) Small molecule inhibitors of the neuropilin-1 vascular endothelial growth factor A (VEGF-A) interaction. J.Med.Chem. 53 2215 PMID: 20151671

Grun et al (2016) VEGF-A acts via neuropilin-1 to enhance epidermal cancer stem cell survival and formation of aggressive and highly vascularized tumors. Oncogene. 35 4379 PMID: 26804163

Miyauchi et al (2016) Ablation of Neuropilin 1 from glioma-associated microglia and macrophages slows tumor progression. Oncotarget. 7 9801 PMID: 26755653

Keywords: EG 00229, EG 00229 supplier, EG00229, antagonists, VEGFA, receptors, neuropilin, nrp1, taxol, increases, chemo, sensitivity, Vascular, endothelial, growth, factor, VEGFR, 4931, Tocris Bioscience

1 Citation for EG 00229

Citations are publications that use Tocris products. Selected citations for EG 00229 include:

Nissen et al (2013) Tuftsin signals through its receptor neuropilin-1 via the transforming growth factor beta pathway. J.Neurochem. 127 394 PMID:  24033337


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Angiogenesis in Cancer

Angiogenesis in Cancer Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.

Pathways for EG 00229

VEGF

VEGF Signaling Pathway

VEGF signaling pathway is involved in embryonic vascular development (vasculogenesis) and in the formation of new blood vessel (angiogenesis). It also induces cell migration, proliferation and survival.