BRN-103
BRN-103 is a nicotinamide derivative and an inhibitor of the VEGF/VEGFR2 angiogenesis signaling pathway. BRN-103 concentration-dependently inhibits VEGF-induced migration, proliferation and capillary-like tube formation of HUVECs, and suppresses microvascular sprouting of ex vivo aortic rings. BRN-103 inhibits VEGF-induced phosphorylation of VEGFR2 Tyr1175, as well as the downstream phosphorylation of AKT Ser473 and eNOS Ser1172, while exerting a weak inhibitory effect on ERK phosphorylation. BRN-103 can be used in studies related to VEGF/VEGFR2 signaling and angiogenesis.
For research use only. We do not sell to patients.
- CAS No.: 1346265-80-2
- Formula: C24H25ClN4O
- Molecular Weight:420.94
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
All VEGFR Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
VEGFR2 |
In Vitro
BRN-103 (0.1-10 μM; 24 h) inhibits VEGF-induced migration of human umbilical vein endothelial cells in Transwell assays in a dose-dependent manner[1].
BRN-103 (0.1-1 μM; 1 h pre-incubation, 24 h incubation with VEGF) inhibits VEGF-induced scratch wound healing migration of human umbilical vein endothelial cells in a dose-dependent manner[1].
BRN-103 (0.1-1 μM) inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs) in a dose-dependent manner[1].
BRN-103 (0.1-1 μM) dose-dependently inhibits VEGF-induced capillary-like tube formation in human umbilical vein endothelial cells[1].
BRN-103 (0.1-1 μM; 1 h pre-incubation, 5 min incubation with VEGFR2) dose-dependently inhibits VEGF-induced phosphorylation of VEGFR2 (Tyr-1175) in human umbilical vein endothelial cells[1].
BRN-103 (0.1-1 μM; 1 h pre-incubation, followed by 5 min, 30 min, or 1 h of incubation with VEGF) dose-dependently inhibits VEGF-induced phosphorylation of AKT (Ser-473) and eNOS (Ser-1172), and slightly inhibits phosphorylation of ERK (Thr-202/Tyr-204) in human umbilical vein endothelial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:human umbilical vein endothelial cells (HUVECs)
-
Concentration:0.1 μM, 0.5 μM, 1 μM
-
Incubation Time:1 h pre-incubation; 5 min incubation with VEGF
-
Result:Dose-dependently suppressed VEGF-induced phosphorylation of VEGFR2 at Tyr-1175 in HUVECs, with greater inhibition observed at higher concentrations.
-
Cell Line:human umbilical vein endothelial cells (HUVECs)
-
Concentration:0.1 μM, 0.5 μM, 1 μM
-
Incubation Time:1 h pre-incubation; 5 min (p-ERK), 30 min (p-AKT), 1 h (p-eNOS) incubation with VEGF
-
Result:Significantly and concentration-dependently suppressed VEGF-triggered phosphorylations of AKT (Ser-473) and eNOS (Ser-1172) in HUVECs.
Mildly inhibited VEGF-induced phosphorylation of ERK (Thr-202/Tyr-204) in HUVECs.
Chemical Information
-
CAS No. 1346265-80-2
-
Molecular Weight 420.94
-
Formula C24H25ClN4O
-
SMILES
O=C(NC=1C=CC=C(Cl)C1)C2=CC=CN=C2NC3CCN(CC=4C=CC=CC4)CC3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BRN-103 Related Classifications
HY-18198 Related Classifications
Powered by Bioz