K5(3-89 ActiveZone)frag SEQ ID NO: 1
General Information
DRACP ID DRACP01765
Peptide Name K5(3-89 ActiveZone)frag SEQ ID NO: 1
Sequence EDCMFGNGKGYRGKRATTVTGTPCQDWAAQEPHRHSIFTPETNPRAGLEKNYCRNPDGDVGGPWCYTTNPRKLYDYCDVPQCAAPKS
Sequence Length 87
UniProt ID P00747
PubChem CID Not available
Origin Not available
Type Synthetic peptide
Classification
Active ACP Cancer targeted peptides
Activity Information
Cell Line | Disease | Cancer Classified | Activity | Assay | Testing Time | Literature |
---|---|---|---|---|---|---|
BT-549 | Invasive breast carcinoma of no special type | Carcinoma | Proliferation Inhibition (5 day) IC50>20000 nM | WST-8 assay | 5 days | Patent |
U-118MG | Astrocytoma | Carcinoma | Proliferation Inhibition (5 day) IC50=49 nM | WST-8 assay | 5 days | Patent |
4T1 | Malignant neoplasms of the mouse mammary gland | Carcinoma | Proliferation Inhibition (5 day) IC50=12529 nM | WST-8 assay | 5 days | Patent |
DA-3 [Mouse lymphoma] | Mouse lymphoma | Lymphoma | Proliferation Inhibition (5 day) IC50=10 nM | WST-8 assay | 5 days | Patent |
DLD-1 | Colon adenocarcinoma | Carcinoma | Proliferation Inhibition (5 day) IC50=380 nM | WST-8 assay | 5 days | Patent |
D-54MG | Glioblastoma | Blastoma | When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 0 ± 5, 12 ± 6, 56 ± 5. | WST-8 assay | 72 h | Patent |
Calu-6 | Lung adenocarcinoma | Carcinoma | When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 7 ± 2, 21 ± 3, 30 ± 4. | WST-8 assay | 72 h | Patent |
MDA-MB-231 | Breast adenocarcinoma | Carcinoma | When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 2 ± 4, 13 ± 2, 46 ± 6. | WST-8 assay | 72 h | Patent |
U-87MG ATCC | Glioblastoma | Blastoma | When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 0 ± 4, 24 ± 5, 64 ± 8. | WST-8 assay | 72 h | Patent |
HT-29 | Colon adenocarcinoma | Carcinoma | When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 0 ± 2, 10 ± 8, 0 ± 10. | WST-8 assay | 72 h | Patent |
Hemolytic Activity Not available
Normal (non-cancerous) Cytotoxicity 293 Kidney fibroblasts: When the concentrations of peptides were 0.1 μg/ml, 1 μg/ml, and 10 μg/ml, the % Proliferation Inhibition was 0 ± 8, 0 ± 10, 0 ± 6.
Target tyrosine kinase orphan receptors (RORs)
Affinity Not available
Mechanism Not available
Nature Anticancer
Structure Information
Helicity Not available
Linear/Cyclic Linear
Disulfide/Other Bond Not available
N-terminal Modification Free
C-terminal Modification Free
Other Modification None
Chiral L
Physicochemical Information
Formula C417H628N124O131S7
Absent amino acids
Common amino acids GPT
Mass 1123289
Pl 7.77
Basic residues 13
Acidic residues 10
Hydrophobic residues 16
Net charge 3
Boman Index -21718
Hydrophobicity -105.06
Aliphatic Index 30.34
Half Life
Mammalian: 30 hour
Yeast: >20 hour
E.coli: >10 hour
Extinction Coefficient cystines 18825
Absorbance 280nm 218.9
Polar residues 35
Amino acid distribution
Literature Information
Literature 1
Pubmed ID Not available
Title Not available
Doi Not available
Year Not available
Patent
Patent ID US2019/0142913A1
Patent Title Grp78 Antagonist That Block Binding of Receptor Tyrosine Kinase Orphan Receptors as Immunotherapy Anticancer Agents
Other Iinformation Patent Application; Family: 2s / 2ex; Family Jurisdictions: US; Legal Status: Active; Application No: 201816184247; Filed: Nov 8, 2018; Published: May 16, 2019; Earliest Priority: Nov 10, 2017; Granted: Feb 2, 2021
Other Published ID US10905750B2