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Submit ReviewEchistatin, α1 isoform is a potent irreversible αVβ3 integrin antagonist (Ki = 0.27 nM). Disrupts attachment of osteoclasts to bone and inhibits bone reabsorption (IC50 = 0.1 nM). Prevents ADP-induced platelet aggregation via inhibition of glycoprotein IIb/IIIa (GpIIb/IIIa, αIIbβ3) receptors (IC50 = 30 nM) in vitro.
M. Wt | 5417.1 |
Formula | C217H341N71O74S9 |
Sequence |
ECESGPCCRNCKFLKEGTICKRARGDDMDDYCNGKTCDCPRNPHKGPAT (Modifications: Disulfide bridges: 2-11, 7-32, 8-37, 20-39) |
Storage | Store at -20°C |
Purity | ≥95% (HPLC) |
CAS Number | 154303-05-6 |
PubChem ID | 90488810 |
InChI Key | KZMZKUVIDVBQGX-UHFFFAOYSA-N |
Smiles | [H]N[C@@H](CCC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]3CSSC[C@@H]4NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H]5CCCN5C(=O)CNC(=O)[C@H](CO)NC(=O)[C@H](CCC(O)=O)NC1=O)C(=O)N3)NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)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](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCCN)NC2=O)[C@@H](C)O)[C@@H](C)CC)[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 | Soluble to 1 mg/ml in water |
References are publications that support the biological activity of the product.
Musial et al (1990) Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins RGD-containing peptides from viper venoms. Circulation 82 261 PMID: 2364514
Sato et al (1990) Echistatin is a potent inhibitor of bone resorption in culture. J.Cell.Biol. 111 1713 PMID: 2211834
Kumar et al (1997) Biochemical characteriation of the binding of echistatin to integrin αVβ3 receptor. J.Pharmacol.Exp.Ther. 283 843 PMID: 9353406
If you know of a relevant reference for Echistatin, α1 isoform, please let us know.
Keywords: Echistatin, alpha1 isoform, Echistatin, alpha1 isoform supplier, αVβ3, alphaVβ3, beta3, glycoprotein, IIb/IIIa, αIIbβ3, alphaIIbβ3, inhibitors, inhibits, Integrin, Receptors, Adhesion, Molecules, Echistatin, alpha1, isoform, Echistatina1, alphavbeta3, Cell, Integrins, 3202, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Echistatin, α1 isoform include:
Lin et al (2013) Angiopoietin-like 3 induces podocyte F-actin rearrangement through integrin α(V)β3/FAK/PI3K pathway-mediated Rac1 activation. PLoS One 2013 135608 PMID: 24294595
Schrader et al (2011) Matrix stiffness modulates proliferation, chemotherapeutic response, and dormancy in hepatocellular carcinoma cells. Biomed Res Int 53 1192 PMID: 21442631
Do you know of a great paper that uses Echistatin, α1 isoform from Tocris? Please let us know.
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