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EXP001289

Paper

Attachment of Cell-Binding Ligands to Arginine-Rich Cell-Penetrating Peptides Enables Cytosolic Translocation of Complexed siRNA (2015)

Peptide

RVG-9LR

Sequence: YTIWMPENPRPGTPCDIFTNSRGKRASNG+RRRRRRRRR

RNA

siRNA

All experiment fields

Experiment Id EXP001289
Paper Attachment of Cell-Binding Ligands to Arginine-Rich Cell-Penetrating Peptides Enables Cytosolic Tran
Peptide RVG-9LR
Delivery Success Class no
In Vivo Flag no
Uptake Confirmed yes
Label Confidence high
In Vitro Functional Effect yes
Endosomal Escape Evidence yes
Peptide Concentration 1–5 µM (ratios 5–25; typically 10:1 used)
Rna Concentration ~200 nM (100 pmol in 0.5 mL for Neuro2a); Jurkat 100 pmol in 0.2 mL (~500 nM)
Mixing Ratio 10:1 (peptide:siRNA molar)
Formulation Format electrostatic peptide:siRNA complex
Formulation Components RVG-9LR + siRNA (noncovalent complex)
Size Nm 203.50
Zeta Mv -28.80
Model Scope in_vitro
Model Type in vitro
Cell Lines Or Primary Cells Neuro2a (mouse neuroblastoma; GFP-expressing)
Animal Model
Administration Route in vitro (cell incubation)
Output Type gene knockdown (GFP reporter)
Output Value GFP-negative cells increased by 69.8 ± 2.7% vs siGFP alone
Output Units
Output Notes Highest uptake at 10:1 (MFI 1,527 ± 121). Rapid cytosolic siRNA translocation and membrane inversion at binding sites; late endosomal release required endosomal proteases.
Toxicity Notes Transient annexin V positivity during membrane inversion without loss of membrane integrity/cytotoxicity (LDH and Alamar Blue assays; data not shown).
Curation Notes