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cHLH-pDI1-R
General Information
DCTPep ID DCTPep02845
Peptide Name cHLH-pDI1-R
Sequence GARELRRLERELRRLEKGGGGGGKLAALTFEHYWAQLTSC
Sequence Length 40
UniProt ID Not available
PubChem CID Not available
Origin Synthetic
Type Synthetic peptide
Classification
Membrane lysis Cell-penetrating peptides
Activity Information
| Cell Line | Disease | Activity | Assay | Testing Time | Literature |
|---|---|---|---|---|---|
| K562 | Blast phase chronic myelogenous leukemia, BCR-ABL1 positive; Chronic myeloid leukemia | CC50>64 μM | Resazurin assay | 26 h | 1 |
| MCF-7 | Invasive breast carcinoma of no special type | CC50>64 μM | Resazurin assay | 26 h | 1 |
| MDA-MB-435S | Amelanotic melanoma | CC50>64 μM | Resazurin assay | 26 h | 1 |
| MM96L | Melanoma | CC50>64 μM | Resazurin assay | 26 h | 1 |
Hemolytic Activity Human erythrocytes: 50% Hemolysis>64 µM
Normal (non-cancerous) Cytotoxicity HFF-1: CC50>64 µM; MCF-10A: CC50>64 µM; Human PBMC: CC50>64 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 DCTPep02845
(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 C195H318N64O56S1
Absent amino acids DIMNPV
Theoretical pI 9.77
Acidic residues 5
Basic residues 9
Polar residues 12
Molecular weight (Average) 4487.13
Molecular weight (Monoisotopic) 4484.37
Common amino acids GL
Net charge 4
Instability index (II) 68.94
Aliphatic index 78.25
Grand average of hydropathicity (GRAVY) -0.677
Half Life
30 hours (mammalian reticulocytes, in vitro).
>20 hours (yeast, in vivo).
>10 hours (Escherichia coli, in vivo).
Extinction coefficients
Ext. coefficient 6990
Abs 0.1% (=1 g/l) 1.558, assuming all pairs of Cys residues form cystines
Ext. coefficient 6990
Abs 0.1% (=1 g/l) 1.558, 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_17188
This work is licensed under a Creative Commons Attribution 4.0 International License.