General
Preferred name
EG 00229
Synonyms
EG 00229 trifluoroacetate ()
EG00229 (trifluoroacetate) ()
EG00229 ()
EG00229 (trifluoroacetate salt) ()
P&D ID
PD038231
CAS
1210945-69-9
1018927-63-3
Tags
available
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
EG00229 is a neuropilin 1 (NRP1) receptor antagonist. EG00229 selectively inhibits VEGF-A binding to NRP1 b1 domain with an IC50 of 3 ¦ÌM, but has no effect on VEGFA binding to VEGFR-1 and VEGFR-2[1].
PRICE
174
DESCRIPTION
EG00229 is a neuropilin 1 (NRP1) receptor antagonist that selectively inhibits the binding of VEGF-A to the NRP1 b1 domain with an IC50 value of 3 ??M. It does not affect the binding of VEGF-A to other receptors, such as VEGFR-1 and VEGFR-2.
DESCRIPTION
EG00229 is a small molecule inhibitor of the binding of VEGF-A165 to its receptor neuropilin 1 (NRP1) . It was originally developed to block neo-vascularisation in tumours. EG00229 has subsequently been used to confirm that NRP1 is a host binding factor for both SARS-CoV and SARS-CoV-2 . It binds directly to the NRP1 domain that binds to the furin-cleaved S1 fragment of the viral spike protein, and by blocking this interaction EG00229 has been shown to reduce viral infection in in vitro systems.
(GtoPdb)
DESCRIPTION
Potent SHMT inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
EG00229 is a small molecule inhibitor of neuropilin-1(Nrp1) with an IC50 of 3μM.
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. (BOC Sciences Bioactive Compounds)
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. (BOC Sciences Bioactive Compounds)
DESCRIPTION
Neuropilin 1 (NRP1) receptor antagonist; inhibits VEGFA binding to NRP1
(Tocriscreen Plus)
DESCRIPTION
EG 00229 is a neuropilin 1 (NRP1) receptor antagonist, inhibiting VEGFA binding to the NRP1 b1 domain.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
8
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Drug Repurposing Hub
Guide to Pharmacology
MedChem Express Bioactive Compound Library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
27
Molecular Weight
497.06
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
6
Rotatable Bonds
10
Ring Count
3
Aromatic Ring Count
3
cLogP
1.0
TPSA
200.25
Fraction CSP3
0.24
Chiral centers
1.0
Largest ring
6.0
QED
0.13
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzyme-Linked Receptors
Primary Target
VEGFR
Target
NRP1
Complement System
MOA
neuropilin receptor antagonist
Pathway
Immunology/Inflammation
Source data
