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Submit ReviewObtustatin
Description: Potent and selective α1β1 inhibitor
Purity: ≥95% (HPLC)
Biological Activity for Obtustatin
Obtustatin is a highly potent integrin α1β1 inhibitor (IC50 = 0.8 nM for α1β1 binding to type IV collagen). Selective for α1β1 over α2β1, αIIbβ3, αvβ3, α4β1, α5β6, α9β1 and α4β7. Inhibits FGF2-stimulated angiogenesis in the chicken chorioallantoic model. Displays antitumor efficacy in a synergistic mouse model of Lewis lung carcinoma; blocks human melanoma growth in nude mice.
Technical Data for Obtustatin
| M. Wt | 4393.07 |
| Formula | C184H284N52O57S8 |
| Sequence |
CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG (Modifications: Disulfide bridges: 1-10, 6-29, 7-34, 19-36) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 404882-00-4 |
| PubChem ID | 90488962 |
| InChI Key | XXWNADNJWWLFFP-UHFFFAOYSA-N |
| Smiles | [H]N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@@H]4NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H]5CCCN5C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC1=O)[C@@H](C)O)[C@@H](C)O)C(=O)N3)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CC1=CNC=N1)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC1=CNC3=C1C=CC=C3)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CC(O)=O)NC4=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N1CCC[C@H]1C(=O)NCC(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC2=O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Obtustatin
| Solubility | Soluble to 1 mg/ml in water |
Product Datasheets for Obtustatin
References for Obtustatin
References are publications that support the biological activity of the product.
Moreno-Murciano et al (2003) Amino acid sequence and homology modeling of obtustatin, a novel non-RGD-containing short disintegrin isolated from the venom of Vipera lebetina obtusa. Protein Sci. 12 366 PMID: 12538900
Marcinkiewicz et al (2003) Obtustatin: a potent and selective inhibitor of α1β1 integrin in vitro and angiogenesis in vivo. Cancer Res. 63 2020 PMID: 12727812
Brown et al (2008) Angiostatic activity of obtustatin as α1β1 integrin inhibitor in experimental melanoma growth. Int.J.Cancer 123 2195 PMID: 18712720
If you know of a relevant reference for Obtustatin, please let us know.
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Keywords: Obtustatin, Obtustatin supplier, integrins, alpha1beta1, a1b1, aαnβ, potent, selective, inhibitors, inhibits, antiangiogenics, angiogenesis, Integrins, Cell, Adhesion, Molecules, Antiangiogenics, 4664, Tocris Bioscience
5 Citations for Obtustatin
Citations are publications that use Tocris products. Selected citations for Obtustatin include:
Elaine T et al (2021) Collagen I Fibrous Substrates Modulate the Proliferation and Secretome of Estrogen Receptor-Positive Breast Tumor Cells in a Hormone-Restricted Microenvironment. ACS Biomater Sci Eng 7 2430-2443 PMID: 33688723
Hanna et al (2017) Modulation of interactions of neuroblastoma cell lines with extracellular matrix proteins affects their sensitivity to treatment with the anti-GD2 ganglioside antibody 14G2a. Int J Oncol 50 1899-1914 PMID: 28393238
Mogami (2018) Collagen Type 1 accelerates healing of ruptured fetal membranes. Sci Rep 8 696 PMID: 29330408
Baghdadi (2018) Reciprocal signalling by Notch-Collagen V-CALCR retains muscle stem cells in their niche Nature 557 714 PMID: 29795344
Elsa et al (2019) The antitumor efficacy of monomeric disintegrin obtustatin in S-180 sarcoma mouse model. Invest New Drugs 37 1044-1051 PMID: 30680583
Do you know of a great paper that uses Obtustatin from Tocris? Please let us know.
Reviews for Obtustatin
Average Rating: 5 (Based on 1 Review.)
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Collagen type 1 activated collagen receptor discoidin domain receptor.
By
Anonymous on 02/21/2020
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: 3D Culture Matrix
10 μg/ml treat 24h and 48h
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Angiogenesis in Cancer Poster
This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
