1. Cell Cycle/DNA Damage
  2. G-quadruplex
  3. DIZ-3

DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells.

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DIZ-3

DIZ-3 Chemical Structure

CAS No. : 2675490-72-7

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Description

DIZ-3 is a selective multimeric G4 ligand based on a G4-ligand-dimerizing strategy. DIZ-3 intercalates into the G4-G4 interface, stabilizing the higher-order structure. DIZ-3 induces cell cycle arrest and apoptosis, and thus inhibits cell proliferation in alternative lengthening of telomere (ALT) cancer cells[1].

Cellular Effect
Cell Line Type Value Description References
BJ IC50
29.3 μM
Compound: DIZ-3
Cytotoxicity against human BJ cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against human BJ cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
[PMID: 31759730]
U2OS IC50
2.1 μM
Compound: DIZ-3
Cytotoxicity against human U2OS cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
Cytotoxicity against human U2OS cells assessed as reduction in cell viability measured after 24 hrs by CCK8 assay
[PMID: 31759730]
In Vitro

DIZ-3 (0-40 μM; 24 hours) inhibits the proliferation in an ALT cancer cell line[1].
DIZ-3 (0.6-2.5 μM; 24 hours) induces U2OS cell cycle arrest and Apoptosis in ALT cancer cells[1].
DIZ-3 (0.12, 0.25, 0.5 μM; 7 days) causes colony formation and would healing assays carried out in U2OS cells[1].
DIZ-3 (0.12, 0.25, 0.5 μM; 24 h) significantly inhibits migration of U2OS cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: Human bone osteosarcoma U2OS cells, normal BJ fibroblasts
Concentration: 0-40 μM
Incubation Time: 24 hours
Result: Caused a significant dose-dependent cytotoxic effect on U2OS cancer cells with an IC50 of 2.1 µM.
Induced much weaker growth inhibition on normal BJ fibroblasts with an IC50 of 29.3 µM.

Apoptosis Analysis[1]

Cell Line: U2OS cells
Concentration: 0.6, 1.2, 2.5 μM
Incubation Time: 24 hours
Result: Induced significant apoptosis in U2OS cells (the percentage of apoptotic cells increased from 10.1% to 24.9%).

Cell Cycle Analysis[1]

Cell Line: U2OS cells
Concentration: 0.6, 1.2, 2.5 μM
Incubation Time: 24 hours
Result: Induced the apparent accumulation of cells in the S phase (increasing from 24.0% to 32.2%) in a dose-dependent manner.
Molecular Weight

746.89

Formula

C46H44F2N8

CAS No.
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)C3=C(NC(C4=CC=C(C=C4)C5=NC(C6=CC=C(C=C6)F)=C(N5)C7=CC=C(C=C7)N8CCN(CC8)C)=N3)C9=CC=C(C=C9)F

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References
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DIZ-3
Cat. No.:
HY-146812
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