1. Others Cell Cycle/DNA Damage Apoptosis GPCR/G Protein MAPK/ERK Pathway
  2. Drug Derivative G-quadruplex Apoptosis Telomerase Ras Bcl-2 Family
  3. G-quadruplex ligand 4

G-quadruplex ligand 4 是一种色原酮衍生物,也是一种人端粒酶逆转录酶 hTERT G4 配体。G-quadruplex ligand 4 会下调 hTERT 的表达,并对三阴性乳腺癌 (TNBC) 细胞系表现出显著的细胞毒性。G-quadruplex ligand 4 可导致 S/G2 期细胞周期停滞并诱导细胞凋亡 (apoptosis)。G-quadruplex ligand 4 会下调 hTERT、KRASBCL-2 的表达。G-quadruplex ligand 4 可用于三阴性乳腺癌的研究。

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G-quadruplex ligand 4

G-quadruplex ligand 4 Chemical Structure

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  • 生物活性

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  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

G-quadruplex ligand 4 (Compound 17) (72 h) 在 MDA-MB-231,HCC-1806,MCF-7 和 HEK-293 细胞中抑制细胞活力,其 IC50 值为 2.5,2.7,5.5 和3.3 μM[1]
G-quadruplex ligand 4 (2.5-10 μM; 72 h) 在 MDA-MB-231 细胞中引起 G2/S 期细胞周期阻滞,并诱导细胞凋亡[1]
G-quadruplex ligand 4 (2.5-10 μM;24 h) 下调 MDA-MB-231 细胞中 hTERT、KRAS 和 BCL-2 的表达[1]。 

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.
分子量

418.53

Formula

C25H30N4O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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G-quadruplex ligand 4
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HY-179480
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