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EXP001598

Paper

Synthesis and Splice-Redirecting Activity of Branched, Arginine-Rich Peptide Dendrimer Conjugates of Peptide Nucleic Acid Oligonucleotides (2010)

Peptide

RXR8-4B1

Sequence: 4-branched dendrimer; total 16 Arg; multiple RXR motifs per arm; C-terminal Ahx-βAla-Cys

RNA

PNA

All experiment fields

Experiment Id EXP001598
Paper Synthesis and Splice-Redirecting Activity of Branched, Arginine-Rich Peptide Dendrimer Conjugates of
Peptide RXR8-4B1
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed no
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence
Peptide Concentration
Rna Concentration
Mixing Ratio
Formulation Format covalent conjugate (disulfide)
Formulation Components RXR8-4B1–PNA705 disulfide conjugate
Size Nm
Zeta Mv
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells A375SM-Luc705-B (melanoma luciferase reporter)
Animal Model
Administration Route
Output Type splice correction / luciferase reporter
Output Value EC50 0.51 ± 0.03 µM (RT-PCR splice correction)
Output Units
Output Notes Assayed in A375SM-Luc705-B melanoma reporter cells; EC50 reported.
Toxicity Notes In A375SM-Luc705-B melanoma cells, cell viability dropped significantly at ≥1 µM for 12- and 16-Arg conjugates (reported for RXR8, RXR8-2B, RXR8-4B1).
Curation Notes