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Submit ReviewObtustatin 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.
分子量 | 4393.07 |
公式 | C184H284N52O57S8 |
序列 |
CTTGPCCRQCKLKPAGTTCWKTSLTSHYCTGKSCDCPLYPG (Modifications: Disulfide bridges: 1-10, 6-29, 7-34, 19-36) |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
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溶解性 | Soluble to 1 mg/ml in water |
参考文献是支持产品生物活性的出版物。
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.
关键词: Obtustatin, Obtustatin supplier, integrins, alpha1beta1, a1b1, aαnβ, potent, selective, inhibitors, inhibits, antiangiogenics, angiogenesis, Integrins, Cell, Adhesion, Molecules, Antiangiogenics, 4664, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Obtustatin 的部分引用包括:
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
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平均评分: 5 (Based on 1 Review.)
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