RGD (Arg-Gly-Asp) Peptides
Synthetic peptides containing the arginine-glycine-aspartate (RGD) were extensively used as inhibitors of integrin-ligand interactions in studies of cell adhesion, migration, growth and differentiation, since the RGD motif is an integrin-recognition motif found in many ligands.
In vitro: RGD peptide can induce apoptosis in the absence of signals and integrin-mediated cell clustering. Previous study demonstrates that RGD peptides promote apoptosis through activation of conformation changes enhancing pro-caspase-3 activation and autoprocessing [1].
In vivo: Anima study suggested that the RGD-4C-FITC-peptide bound to both endothelial and tumor cells in vivo and that peptide targeting should allow the delivery of therapeutic drugs to both endothelial and tumor cells [2].
Clinical trials: Currenlty no clinical data are available.
References:
[1] Nature. 1999 Feb 11;397(6719):534-9.
RGD peptides induce apoptosis by direct caspase-3 activation.
Buckley CD1, Pilling D, Henriquez NV, Parsonage G, Threlfall K, Scheel-Toellner D, Simmons DL, Akbar AN, Lord JM, Salmon M.
[2] Cancer Res. 2002 Sep 15;62(18):5139-43. Arginine-glycine-aspartic acid (RGD)-peptide binds to both tumor and tumor-endothelial cells in vivo. Zitzmann S1, Ehemann V, Schwab M.
- 1. Xining Li, Jianyou Li, et al. "The role of T cell related genes in COVID-19 and osteoporosis and the screening of biomarkers were explored based on bioinformatics." Advance. September 03, 2024.
- 2. Lee HN, Bosompra OA, Coller HA. "RECK isoforms differentially regulatefibroblast migration by modulating tubulin post-translational modifications."Biochem Biophys Res Commun. 2019 Mar 5;510(2):211-218. PMID:30704758
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 346.34 |
| Cas No. | 99896-85-2 |
| Formula | C12H22N6O6 |
| Solubility | insoluble in DMSO; insoluble in EtOH; ≥17.3 mg/mL in H2O with gentle warming |
| SDF | Download SDF |
| Canonical SMILES | C(CC(C(=O)NCC(=O)NC(CC(=O)O)C(=O)O)N)CN=C(N)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
Lung fibroblasts |
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Preparation method |
The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
1 mM; 24 hrs |
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Applications |
In lung fibroblasts, RGD peptides induced apoptosis and caspase-3 activation. Moreover, in both adherent and detached cells, RGD peptides resulted in pro-caspase-3 cleavage. Thus, RGD-containing peptides can induce apoptosis before the adherent cells detach from their substrates. |
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References: [1]. Buckley CD, Pilling D, Henriquez NV, Parsonage G, Threlfall K, Scheel-Toellner D, Simmons DL, Akbar AN, Lord JM, Salmon M. RGD peptides induce apoptosis by direct caspase-3 activation. Nature. 1999 Feb 11;397(6719):534-9. |
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| Description | RGD is an inhibitor of integrin-ligand interactions. | |||||
| Targets | integrin-ligand interaction | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
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