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  2. Drug Derivative G-quadruplex Apoptosis Telomerase Ras Bcl-2 Family
  3. G-quadruplex ligand 4

G-quadruplex ligand 4 is a chromenone derivative and is a human telomerase reverse transcriptase (hTERT) G4 ligand. G-quadruplex ligand 4 downregulates hTERT expression and exhibits notable cytotoxicity towards triple-negative breast cancer (TNBC) cell lines. G-quadruplex ligand 4 can cause S/G2 cell cycle arrest and induce apoptosis. G-quadruplex ligand 4 downregulates the expression of hTERT, KRAS, and BCL-2. G-quadruplex ligand 4 can be used for the research of TNBC.

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G-quadruplex ligand 4

G-quadruplex ligand 4 Chemical Structure

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Description

G-quadruplex ligand 4 is a chromenone derivative and is a human telomerase reverse transcriptase (hTERT) G4 ligand. G-quadruplex ligand 4 downregulates hTERT expression and exhibits notable cytotoxicity towards triple-negative breast cancer (TNBC) cell lines. G-quadruplex ligand 4 can cause S/G2 cell cycle arrest and induce apoptosis. G-quadruplex ligand 4 downregulates the expression of hTERT, KRAS, and BCL-2. G-quadruplex ligand 4 can be used for the research of TNBC[1].

IC50 & Target[1]

Bcl-2

 

K-RAS

 

In Vitro

G-quadruplex ligand 4 (Compound 17) (72 h) inhibits cell viability in MDA-MB-231, HCC-1806, MCF-7 and HEK-293 with IC50 values of 2.5, 2.7 , 5.5 and 3.3 μM[1].
G-quadruplex ligand 4 (2.5-10 μM; 72 h) causes G2/S phase cell cycle arrest and induces apoptosis in MDA-MB-231 cells[1].
G-quadruplex ligand 4 (2.5-10 μM; 24 h) downregulates the expression of hTERT, KRAS, and BCL-2 in MDA-MB-231 cells[1]

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

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Showed increasing proportions of early-apoptotic (4.9%, 9.5%, 28.8%) and late-apoptotic cells (12.1%, 17.4%, 30.0%) at different concentrations.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration:  2.5 μM, 5 μM, 10 μM
Incubation Time: 72 h
Result: Increased the proportion of cells in the S phase (17.5%, 23.9%, 29.0%) and G2 phase (11.1%, 16.1%, 23.7%). 

Real Time qPCR[1]

Cell Line: MDA-MB-231 cells
Concentration:  2.5 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Showed significant reductions in mRNA levels with KRAS (21-23 %), BCL-2 (25-30 %), and hTERT (40-56 %); \r
whereas the expression of HRAS and c-MYC remained unchanged.
Molecular Weight

418.53

Formula

C25H30N4O2

SMILES

CN1CCN(CC1)C2=CC=C(C=C2)C3=CC(C4=C(O3)C=CC(N5CCN(CC5)C)=C4)=O

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Room temperature in continental US; may vary elsewhere.

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G-quadruplex ligand 4
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HY-179480
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