Cyclo(-Pro-Val) is a diketopiperazines which shows antifungal activity, has also been isolated from microorganisms and further natural sources. Cyclo(-Pro-Val) is also capable of activating or antagonizing other LuxR-based quorum-sensing systems. While the mode of action of the cyclo(L-Pro-L-Val) is not known, its activity suggests the existence of cross talk among bacterial signaling systems.
Cyclo(-RGDfK) TFA is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[3].
IC50 & Target
IC50: 0.94 nM (αvβ3 integrin)[1]
体外研究 (In Vitro)
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin and exhibits a IC50 of 0.94 nM[1].[66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
717.69
Formula
C29H42F3N9O9
CAS 号
500577-51-5
Sequence Shortening
Cyclo(RGDFK)
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Simecek J, et al. Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK). Mol Pharm. 2014 May 5;11(5):1687-95.
[2]. Lopez-Rodriguez V, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14.
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with an IC50 of 0.94 nM[1]. Cyclo(-RGDfK) TFA potently targets tumor microvasculature and cancer cells through the specific binding to the αvβ3 integrin on the cell surface[2].
IC50 & Target
IC50: 0.94 nM (αvβ3 integrin)[1].
体外研究 (In Vitro)
Cyclo(-RGDfK) is a potent and selective inhibitor of the αvβ3 integrin, with a IC50 of 0.94 nM[1]. [66Ga]DOTA-E-[c(RGDfK)]2 can be prepared with high radiochemical purity (>97%), specific activity (36-67GBq/μM), in vitro stability, and moderate protein binding. MicroPET imaging up to 24 post-injection showed contrasting tumors reflecting αvβ3-targeted tracer accumulation[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
603.67
Formula
C27H41N9O7
CAS 号
161552-03-0
Sequence Shortening
Cyclo(RGDFK)
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Simecek J, et al. Benefits of NOPO as chelator in gallium-68 peptides, exemplified by preclinical characterization of (68)Ga-NOPO-c(RGDfK). Mol Pharm. 2014 May 5;11(5):1687-95.
[2]. Lopez-Rodriguez V, et al. Preparation and preclinical evaluation of (66)Ga-DOTA-E(c(RGDfK))2 as a potential theranostic radiopharmaceutical. Nucl Med Biol. 2015 Feb;42(2):109-14.
This peptide is a negative control for the cyclo (-RGDfE) peptide. RGD peptides are modulators of cell adhesion, and are recognized by several members of the integrin family. This peptide has a low affinity binding to integrin peptides.
溶解度
分子量
569.6
化学式
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Mogford, JE. et al. Circulation Res. 79, 821 (1996)
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Van Hagen, PM. et al. Int. J. Cancer 90, 186 (2000) Hu, B. et al. Biochem. 39, 2284 (2000). M. Kantlehner, et al., Chembiochem., 1, 107 (2000). R.J. Kok, et al., Bioconjug. Chem., 13, 128 (2002).
Synthetic peptide that mimics the structure of a 38-amino acid unit from a staphylococcal fibronectin-binding protein. This peptide represents the protein domain to which the fibronectin-binding activity has been localized and also inhibits binding of fibronectin to bacterial cells.
溶解度
分子量
876.96
化学式
C38H60N12O12
存储条件
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
Van Hagen, PM. et al. Int. J. Cancer 90, 186 (2000) Hu, B. et al. Biochem. 39, 2284 (2000). M. Kantlehner, et al., Chembiochem., 1, 107 (2000). R.J. Kok, et al., Bioconjug. Chem., 13, 128 (2002).
Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference
R. Haubner, et al., J. Nuclear Med., 42, 326 (2001). X. Chen, et al., Nucl. Med. Biol., 31, 179 (2004). X. Chen, et al., Cancer Res., 641, 8009 (2004).
Cyclo(Ala-Gly), a metabolite of a mangrove endophytic fungus, Penicillium thomi, exhibits cytotoxicity against A549, HepG2 and HT29 cells. The IC50 values range from 9.5 to 18.1 μM[1].
分子量
128.13
Formula
C5H8N2O2
CAS 号
4526-77-6
运输条件
Room temperature in continental US; may vary elsewhere.
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM[1].
体外研究 (In Vitro)
TAT-cyclo-CLLFVY inhibits HIF-1 activity in a mammalian cell luciferase reporter assay[1]. Hypoxia (1% O2) results in a ~12-fold increase in the luciferase signal, which is inhibited in a dose-dependent manner by TAT-cyclo-CLLFVY (IC50 of 19±2 μM)[1]. To assess the cell-specificity of TAT-cyclo-CLLFVY, the experiment is repeated in MCF-7 breast cancer cells with similar results (TAT-cyclo-CLLFVY IC50 of 16±1 μM)[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
[1]. Elena Miranda, et al. A cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. J Am Chem Soc. 2013 Jul 17;135(28):10418-25.