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].
MCE 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.
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].
MCE 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(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis.
IC50 Target
Integrin[1].
体外研究 (In Vitro)
Cyclo(RADfK) is a negative control for the cyclo (-RGDfK-), the RGD peptide. RGD peptides are modulators of cell adhesion and are recognized by several members of the integrin family[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
617.70
Formula
C28H43N9O7
CAS 号
756500-23-9
Sequence Shortening
Cyclo(ADFKR)
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Srivatsan A, et al. Conjugation of cRGD peptide to chlorophyll a based photosensitizer (HPPH) alters its pharmacokinetics withenhanced tumor-imaging and photosensitizing (PDT) efficacy. Mol Pharm. 2011 Aug 1;8(4):1186-1197.