154303-05-6
Chemical Structure
Echistatin
- CAS No.: 154303-05-6
- Formula:C217H341N71O74S9
- Molecular Weight:5417.00
SMILES: O=C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H](CCC(O)=O)C(NCC(N[C@@H]([C@H](O)C)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CSSC[C@@H](C(N2[C@@H](CCC2)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(N)=O)C(N3[C@@H](CCC3)C(N[C@@H](CC4=CNC=N4)C(N[C@@H](CCCCN)C(NCC(N5[C@@H](CCC5)C(N[C@@H](C)C(N[C@@H]([C@H](O)C)C(O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC6=O)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@@H](CCCNC(N)=N)C(NCC(N[C@@H](CC(O)=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@@H](CC(O)=O)C(N[C@H]7CC8=CC=C(C=C8)O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)NC9=O)C(N[C@@H](CCC(O)=O)C(N[C@@H](CO)C(NCC(N%10[C@@H](CCC%10)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CC(N)=O)C(NCC(N[C@@H](CCCCN)C(N[C@H]%11[C@H](O)C)=O)=O)=O)=O)NC7=O)C(N[C@@H](CSSC[C@@H](C(N[C@H]6CC(O)=O)=O)NC%11=O)C(N[C@@H](CCCNC(N)=N)C(N[C@H]9CC(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCC(O)=O)N
Biological Activity: Echistatin is a naturally derived RGD-containing snake venom peptide. Echistatin exhibits an IC50 of 0.6 nM against mouse αvβ3 integrin, and acts as an antagonist against αvβ3, αIIbβ3, α5β1 integrins, pp125FAK and paxillin. Echistatin reduces the phosphorylation of pp125FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125FAK, and weakens its binding to pp60src and paxillin. Echistatin disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism[1][2][3][4].
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Echistatin | 91.33% | Echistatin is a naturally derived RGD-containing snake venom peptide. Echistatin exhibits an IC50 of 0.6 nM against mouse αvβ3 integrin, and acts as an antagonist against αvβ3, αIIbβ3, α5β1 integrins, pp125FAK and paxillin. Echistatin reduces the phosphorylation of pp125FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125FAK, and weakens its binding to pp60src and paxillin. Echistatin disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin inhibits osteoclast maturation and migration, bone resorption, platelet aggregation, bone loss, as well as adhesion and metastasis of Lewis lung cancer cells; it also increases the number of osteoclasts and bone coverage area in mice with secondary hyperparathyroidism. Echistatin can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism. | ||||||||||||||||||||
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- [1]. Della Morte R, et al. Echistatin inhibits pp125FAK autophosphorylation, paxillin phosphorylation and pp125FAK-paxillin interaction in fibronectin-adherent melanoma cells. European journal of biochemistry. 2000 Aug;267(16):5047-54. [Content Brief]
- [2]. Nakamura I, et al. Echistatin inhibits the migration of murine prefusion osteoclasts and the formation of multinucleated osteoclast-like cells. Endocrinology. 1998 Dec;139(12):5182-93. [Content Brief]
- [3]. Masarachia P, et al. Histomorphometric evidence for echistatin inhibition of bone resorption in mice with secondary hyperparathyroidism. Endocrinology. 1998 Mar;139(3):1401-10. [Content Brief]
- [4]. Spalleticernia D, et al. Echistatin inhibits Lewis lung carcinoma cell-matrix adhesion in vitro and experimental metastasis in vivo. International journal of oncology. 1997 Oct;11(4):757-63. [Content Brief]
Keywords