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.
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- CAS. Nr.: 1346265-80-2
- Formel: C24H25ClN4O
- Molecular Weight:420.94
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:0.1 μM, 0.5 μM, 1 μM
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Incubation Time:1 h pre-incubation; 5 min incubation with VEGF
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Result:Dose-dependently suppressed VEGF-induced phosphorylation of VEGFR2 at Tyr-1175 in HUVECs, with greater inhibition observed at higher concentrations.
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Cell Line:human umbilical vein endothelial cells (HUVECs)
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Concentration:0.1 μM, 0.5 μM, 1 μM
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Incubation Time:1 h pre-incubation; 5 min (p-ERK), 30 min (p-AKT), 1 h (p-eNOS) incubation with VEGF
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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
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CAS. Nr. 1346265-80-2
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Molecular Weight 420.94
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Formel C24H25ClN4O
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SMILES
O=C(NC=1C=CC=C(Cl)C1)C2=CC=CN=C2NC3CCN(CC=4C=CC=CC4)CC3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
BRN-103 Related Classifications
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