Echistatin TFA
Based on 1 Customer Validation
Echistatin TFA is a naturally derived RGD-containing snake venom peptide. Echistatin TFA 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 TFA reduces the phosphorylation of pp125FAK and paxillin, inhibits the autophosphorylation and kinase activity of pp125FAK, and weakens its binding to pp60src and paxillin. Echistatin TFA disrupts the actin cytoskeleton and focal adhesions, induces melanoma cell detachment from fibronectin, and regulates cell adhesion and motility. Echistatin TFA 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 TFA can be used in research related to melanoma, lung cancer and secondary hyperparathyroidism.
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- Pureté: 99.32%
- Formule: C217H341N71O74S9.xC2HF3O2
- Masse moléculaire:5417.00 (free acid)
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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αvβ3 |
α5β1 |
αIIbβ3 |
Echistatin (100 μg/mL; 15 min-3 h) TFA reduces the phosphorylation level of pp125FAK Tyr397 in fibronectin-adherent B16-BL6 mouse melanoma cells; decreases the binding level of pp125FAK to paxillin in a time-dependent manner; and inhibits the autophosphorylation of pp125FAK, the phosphorylation of paxillin, and the binding level of pp125FAK to pp60src[1].
Echistatin (100 μg/mL; 30 min) TFA induces detachment of fibronectin-adherent B16-BL6 mouse melanoma cells and causes loss of pp125FAK and paxillin from focal adhesions[1].
Echistatin (10 nCi/tube; 1 h) TFA binds specifically to αvβ3 integrin in membrane fractions enriched from mouse osteoclast-like cells, with an IC50 of 0.6 nM, and this binding is selectively blocked by anti-αvβ3 integrin antibody[2].
Echistatin (100 nM; 7 days, days 0-4, days 4-7) TFA potently inhibits the formation of TRAP-positive multinucleated osteoclast-like cells in a mouse MB1.8 cell-bone marrow co-culture system, with an IC50 of 0.7 nM[2].
Echistatin (10-11 to 10-8 M; 15 h) TFA inhibits M-CSF-induced fusion of mouse mononuclear pre-fusion osteoclasts with an IC50 of 0.6 nM, and inhibits M-CSF-induced migration of mouse mononuclear pre-fusion osteoclasts with an IC50 of 1.0 nM[2].
Echistatin TFA enables the quantitative detection of Echistatin levels in biological samples via competitive receptor binding assays, in which Echistatin extracts from HEK 293 cells overexpressing αvβ3 integrin displace radiolabeled Echistatin[3].
Echistatin (0.1-20 μg/mL; 10 min-6 days) TFA is a reversible, non-cytotoxic inhibitor that suppresses the adhesion of Lewis lung carcinoma (3LL) cells to immobilized fibronectin and laminin in vitro[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Echistatin (6-30 µg/kg/min; subcutaneous injection; continuous infusion; 6 h) TFA inhibits the acute calcemic response to exogenous PTH in parathyroidectomized mice[3].
Echistatin (20 μg; intramuscular injection; co-injected once together with tumor cells) TFA co-administrated with 2.5 × 105 3LL cells via intramuscular injection suppresses tumor growth and metastasis of Lewis lung carcinoma in male C57BL/6NCrlBR mice[4].
Echistatin (1 μg/g; intraperitoneal injection; once every 72 hours; 4 doses total) TFA inhibits Lewis lung cancer tumor growth and metastasis formation in male C57BL/6NCrlBR mice[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Masse moléculaire 5417.00 (free acid)
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Formule C217H341N71O74S9.xC2HF3O2
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Color White to off-white
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Sequence
Glu-Cys-Glu-Ser-Gly-Pro-Cys-Cys-Arg-Asn-Cys-Lys-Phe-Leu-Lys-Glu-Gly-Thr-Ile-Cys-Lys-Arg-Ala-Arg-Gly-Asp-Asp-Met-Asp-Asp-Tyr-Cys-Asn-Gly-Lys-Thr-Cys-Asp-Cys-Pro-Arg-Asn-Pro-His-Lys-Gly-Pro-Ala-Thr (Disulfide bridge:Cys2-Cys11;Cys7-Cys32;Cys8-Cys37;Cys20-Cys39)
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Sequence Shortening
ECESGPCCRNCKFLKEGTICKRARGDDMDDYCNGKTCDCPRNPHKGPAT (Disulfide bridge:Cys2-Cys11;Cys7-Cys32;Cys8-Cys37;Cys20-Cys39)
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Structure Classification
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Initial Source
snake venoms
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
H2O : 50 mg/mL (Need ultrasonic)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL; Clear solution; Need ultrasonic
Pureté et documentation
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Fiche technique (308 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Echistatin TFA Related Classifications
HY-P1189A Related Classifications
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