VEGF Inhibitor, V1 - Calbiochem (C15-1307-621)

General description

An NRP-1-binding heptapeptide whose target was initially mistaken as VEGFR2/KDR/Flk-1 due to its binding activity to a CHO-KDR culture that was later shown to express primarily NRP-1 and little KDR. V1/A7R specifically competes against VEGF₁₆₅ binding to recombinant NRP-1 in cell-free binding assays (IC₅₀ = 60 µM), while exhibiting no activity against the interaction between NRP-1 and heparin or VEGF₁₆₅ binding to KDR, VEGFR1/Flt-1, and heparin. V1/A7R is demonstrated to inhibit VEGF-dependent angiogenesis activity in HMVEC (IC₅₀ = 0.3 µM) and HUVEC cultures in vitro, as well as in a rabbit corneal neovascularization model and in mice bearing MDA-MB-231-derived tumor in vivo.

An NRP-1-binding heptapeptide whose target was initially mistaken as VEGFR2/KDR/Flk-1 due to its binding activity to a CHO-KDR culture that was later shown to express primarily NRP-1 and little KDR. V1/A7R specifically competes against VEGF₁₆₅ binding to recombinant NRP-1 in cell-free binding assays (IC₅₀ = 60 µM), while exhibiting no activity against the interaction between NRP-1 and heparin or VEGF₁₆₅ binding to KDR, VEGFR1/Flt-1, and heparin. V1/A7R is demonstrated to inhibit VEGF-dependent angiogenesis activity in HMVEC (IC₅₀ = 0.3 µM) and HUVEC cultures in vitro, as well as in a rabbit corneal neovascularization model and in mice bearing MDA-MB-231-derived tumor in vivo.

Biochem/physiol Actions

Cell permeable: no

Primary Target
Specifically competes against VEGF165 binding to recombinant NRP-1

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 60 µM for specifically competes against VEGF165 binding to recombinant NRP-1 in cell-free binding assays

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

H-Ala-Thr-Trp-Leu-Pro-Pro-Arg-OH

Other Notes

Starzec, A., et al. 2006. Life Sci.79, 2370.
Binetruy-Tournaire, R., et al. 2000. EMBO J.19, 1525.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Molecular Weight: 839.98. Empirical Formula: C₄₀H₆₁N₁₁O₉. Quality Level: 100. Assay: ≥. 95% (HPLC). form: lyophilized solid. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic). color: white. solubility: DMSO: 5 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.