Peptide Libraray

[G17K]cHLH-p53R

General Information

DCTPep ID DCTPep02844

Peptide Name [G17K]cHLH-p53R

Sequence GARELRRLERELRRLEKGGGGGGKLAALKFKLLWLKLAC

Sequence Length 39

UniProt ID Not available

PubChem CID Not available

Origin Synthetic

Type Synthetic peptide

Classification

ACP Tumor active peptide Membrane lysis Cell-penetrating peptides

Activity Information

Cell Line	Disease	Activity	Assay	Testing Time	Literature
MM96L	Melanoma	CC50=5.3 ± 0.5 μM	Resazurin assay	26 h	1
MDA-MB-435S	Amelanotic melanoma	CC50=7.1 ± 0.6 μM	Resazurin assay	26 h	1

Hemolytic Activity Human erythrocytes: 50% Hemolysis>64 µM

Normal (non-cancerous) Cytotoxicity HFF-1: CC50=8.8 ± 1.2 µM; MCF-10A: CC50=25.7 ± 3.2 µM; Human PBMC: CC50=42.8 ± 7.0 µM

Target Not available

Affinity Not available

Mechanism (1) The positively charged peptide targets the negative surface of cancer cells via electrostatic attractions; (2) The peptide inserts into cell membranes and enters inside cells very efficaciously; (3) Once inside cells, the peptide induces toxicity through fusion and/or disruption of intracellular organelles; (4) The cell membrane is disrupted and the cells die.

Structure Information

PDB ID Not available

Predicted Structure DCTPep02844

(Please note that there is the predicted structure, predicted by AlphaFold)

Helicity Not available

Linear/Cyclic Cyclic

Disulfide/Other Bond TIE: N-terminal Chloroacetic acid<--->Cys39

N-terminal Modification CAA, Chloroacetic acid

C-terminal Modification Free

Other Modification None

Chiral L

Physicochemical Information

Formula C195H337N63O48S1

Absent amino acids DHIMNPQSTVY

Theoretical pI 10.96

Acidic residues 4

Basic residues 11

Polar residues 8

Molecular weight (Average) 4364.27

Molecular weight (Monoisotopic) 4361.56

Common amino acids L

Net charge 7

Instability index (II) 64.05

Aliphatic index 110.26

Grand average of hydropathicity (GRAVY) -0.351

Half Life
30 hours (mammalian reticulocytes, in vitro).
>20 hours (yeast, in vivo).
>10 hours (Escherichia coli, in vivo).

Extinction coefficients
Ext. coefficient 5500
Abs 0.1% (=1 g/l) 1.260, assuming all pairs of Cys residues form cystines
Ext. coefficient 5500
Abs 0.1% (=1 g/l) 1.260, assuming all Cys residues are reduced

Amino acid distribution

Literature Information

Literature 1

Pubmed ID 31390185

Title Cell Membrane Composition Drives Selectivity and Toxicity of Designed Cyclic Helix-Loop-Helix Peptides with Cell Penetrating and Tumor Suppressor Properties

Doi 10.1021/acschembio.9b00593

Year 2019

Patent

Patent ID Not available

Patent Title Not available

Other Iinformation Not available

Other Published ID Not available

External Code

DBAASP ID DBAASPS_17187