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SPMI-HIF2-3
General Information
DRACP ID DRACP05916
Peptide Name SPMI-HIF2-3
Sequence TSFⓍEYWALLⓍXLAXYXP
Sequence Length 18
UniProt ID Not available
PubChem CID Not available
Origin Synthetic
Type Synthetic peptide
Classification
Cancer targeted peptides Stapled Peptides Induce apoptosis Induce cell cycle arrest MDM6/MDMX Inhibitor
Activity Information
| Cell Line | Disease | Cancer Classified | Activity | Assay | Testing Time | Literature |
|---|---|---|---|---|---|---|
| HCT 116 p53+/+ | Colon carcinoma | Carcinoma | IC50=15.2 μM | CCK-8 assay | 72 h | 1 |
| HCT 116 p53-/- | Colon carcinoma | Carcinoma | IC50>100 μM | CCK-8 assay | 72 h | 1 |
Hemolytic Activity Not available
Normal (non-cancerous) Cytotoxicity Not available
Target MDM2, MDMX
Affinity Not available
Mechanism Not available
Nature Anticancer
Structure Information
Helicity 24
Linear/Cyclic Cyclic (Stapled)
Disulfide/Other Bond Stapled: Ⓧ(4) and Ⓧ (11) are cross-linked by hydrocarbon stapling
N-terminal Modification Acetylation
C-terminal Modification Amidation
Other Modification Ⓧ(4)=R-octenyl-alanine; Ⓧ(11)=S-pentenyl-alanine; X(12)=Peg3, polyethylene glycol; X(15)=Hyp, hydroxyproline; X(17)=Hle, homoleucine
Chiral L
Physicochemical Information
Formula C79H98N14O15
Absent amino acids CDGHIKMNQRV
Common amino acids LX
Mass 211713
Pl 3.85
Basic residues 0
Acidic residues 1
Hydrophobic residues 7
Net charge -1
Boman Index 1063
Hydrophobicity 42.78
Aliphatic Index 76.11
Half Life
/
Extinction Coefficient cystines 8480
Absorbance 280nm 498.82
Polar residues 4
Amino acid distribution
Literature Information
Literature 1
Pubmed ID 36185610
Title Design of stapled peptide-based PROTACs for MDM2/MDMX atypical degradation and tumor suppression
Year 2022
Patent
Patent ID Not available
Patent Title Not available
Other Iinformation Not available
Other Published ID Not available
This work is licensed under a Creative Commons Attribution 4.0 International License.