EG 00229

Pricing Availability Delivery Time Qty
Cat.No. 4931 - EG 00229 | C17H19N7O5S3 | CAS No. 1018927-63-3
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)
Literature
Pathways

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. NaOH 49.76 100
DMSO 49.76 100

Preparing Stock Solutions

The following data is based on the product molecular weight 497.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.01 mL 10.05 mL 20.1 mL
5 mM 0.4 mL 2.01 mL 4.02 mL
10 mM 0.2 mL 1 mL 2.01 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


If you know of a relevant reference for EG 00229, please let us know.

Keywords: EG00229 antagonists VEGFA receptors neuropilin nrp1 taxol increases chemo sensitivity Vascular endothelial growth factor VEGFR

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


Do you know of a great paper that uses EG 00229 from Tocris? If so please let us know.

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Reviews

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Literature in this Area

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.

Protocols

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