2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis Topoisomerase
  4. Topoisomerase I/II-IN-9

Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer.

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Topoisomerase I/II-IN-9

Topoisomerase I/II-IN-9 Chemical Structure

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Topoisomerase I/II-IN-9 Related Antibodies

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Topoisomerase Topo I Topo II DNA gyrase

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Description

Topoisomerase I/II-IN-9 is a topoisomerase I/II inhibitor (IC50<10 μM) and a DNA damage inducer. Topoisomerase I/II-IN-9 blocks the interaction between the enzyme and DNA by binding to the DNA-binding pocket of the enzyme. Topoisomerase I/II-IN-9 activates the cGAS-STING pathway and promotes the accumulation of cytoplasmic double-stranded DNA. This further drives the production of type I interferons, CCL5, CXCL10 and interferon-stimulated genes, and induces anti-tumor immune responses in vivo. Topoisomerase I/II-IN-9 can be applied to the research of related diseases such as triple-negative breast cancer, colorectal cancer and gastric cancer[1].

IC50 & Target

Topoisomerase I

<10 μM (IC50)

Topoisomerase II

<10 μM (IC50)

In Vitro

Topoisomerase I/II-IN-9 (Ru-4) exhibits potent in vitro antiproliferative activity against CT26, MGC-803, MDA-MB-231, and 4T1 cancer cells, with the highest potency against 4T1 cells (24 h, IC50=1.09 μM)[1].
Topoisomerase I/II-IN-9 (IC50; 48 h) induces DNA double-strand breaks in 4T1 mouse triple negative breast cancer cells[1].
Topoisomerase I/II-IN-9 (IC50; 0-48 h) activates the cGAS-STING-TBK1-IRF3 axis in a time-dependent manner in 4T1 mouse triple negative breast cancer cells, and this activation is required for the induced upregulation of CCL5 and CXCL10[1].
Topoisomerase I/II-IN-9 (IC50; 0-48 h) induces time-dependent upregulation of phosphorylated STAT1 in 4T1 mouse triple negative breast cancer cells, with significant activation observed by 24 h of treatment[1].
Topoisomerase I/II-IN-9 (IC50; 0-48 h) induces time-dependent upregulation of CCL5 and CXCL10 expression and secretion in 4T1 mouse triple negative breast cancer cells, with maximum secretion of ~135 pg/mL CCL5 and ~2400 pg/mL CXCL10 at 48 h[1].
Topoisomerase I/II-IN-9 (1.2-4.8 μM; 48 h; IC50; 0-48 h) upregulates IFN-β and ISG15 mRNA expression in a concentration- and time-dependent manner in 4T1 mouse triple negative breast cancer cells[1].
Topoisomerase I/II-IN-9 (1.2-4.8 μM; 48 h) stimulates concentration-dependent secretion of IFN-β protein in 4T1 mouse triple negative breast cancer cells, with maximum secretion of ~16 U/mL at 4.8 μM[1].

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

Topoisomerase I/II-IN-9 Related Antibodies

Immunofluorescence[1]

Cell Line: 4T1 mouse triple negative breast cancer cells
Concentration: IC50
Incubation Time: 48 h
Result: Induced a notable increase in γ-H2AX fluorescence intensity compared to untreated controls.
Confirmed the induction of DNA double-strand breaks.

Real Time qPCR[1]

Cell Line: 4T1 mouse triple negative breast cancer cells
Concentration: 1.2, 1.8, 2.4, 3.6, 4.8 μM; IC50
Incubation Time: 48 h (1.2, 1.8, 2.4, 3.6, 4.8 μM); 0, 12, 24, 36, 48 h (IC50)
Result: Upregulated IFN-β and ISG15 mRNA levels in a concentration-dependent manner.
Upregulated IFN-β and ISG15 mRNA levels in a time-dependent manner.
Caused statistically significant increases at all tested concentrations and time points relative to untreated controls.

ELISA Assay[1]

Cell Line: 4T1 mouse triple negative breast cancer cells
Concentration: 1.2, 1.8, 2.4, 3.6, 4.8 μM
Incubation Time: 48 h
Result: Increased IFN-β secretion in a concentration-dependent manner.
Caused statistically significant increases at all tested concentrations relative to untreated controls.
Reached a maximum level of ~16 U/mL at 4.8 μM.
In Vivo

Topoisomerase I/II-IN-9 (Ru-4) (10-30 mg/kg; i.v.; every 2 days) is well-tolerated at doses up to 20 mg/kg in Kunming mice, while the 30 mg/kg dose causes significant weight loss[1].
Topoisomerase I/II-IN-9 (20 mg/kg; i.v.; every 2 days) exhibits potent in vivo antitumor activity in female BALB/c mice bearing 4T1 tumors, with a 36.7% tumor growth inhibition rate, activates the cGAS-STING pathway, and enhances antitumor immune responses by increasing effector T cell populations and reducing regulatory T cells[1].

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

Animal Model: BALB/c (female, 4T1 tumor cells implanted when tumor diameter reached 20 mm3)[1]
Dosage: 20 mg/kg
Administration: i.v.; every 2 days
Result: Inhibited 4T1 tumor growth with a 36.7% tumor growth inhibition rate, which was higher than the inhibition rates of cisplatin (18.4%) and anti-PD1 (13.9%) alone.
Induced only modest body weight loss, compared to significant weight loss in cisplatin-treated mice.
Upregulated tumor expression of p-STING (7.56-fold increase), p-IRF3 (5.85-fold increase), CXCL10 (5.52-fold increase), and CCL5 (6.98-fold increase) relative to controls.
Increased the percentage of CD3+CD8+ T cells to 2.21%, CD3+CD8+Ki67+ T cells to 55.54%, and CD3+CD8+CD38+ T cells to 46.99%.
Increased the percentage of CD3+CD4+ T cells to 7.42% and CD4+CD185+ (Th) cells to 31.66%.
Reduced tumor CD3+CD4+Foxp3+ (Treg) cells to 2.19%.
Increased expression of TNF-α (5.58%), IFN-γ (10.80%), and GZMB (5.81%) in tumor CD3+CD8+ T cells (from 0.14%, 0.44%, and 0.28% in controls, respectively).
Molecular Weight

761.72

Formula

C35H37F6N3OPRu
SMILES

C[Ru]1([N]2=CC=C(N(C)C)C=C2)[N](C=C3)=C4C5=C(C=CC=C51)C(C6=CC=CC3=C64)=O.CC7=CC=C(C(C)(C)C)C=C7.F[P-](F)(F)(F)(F)F
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Topoisomerase I/II-IN-9 Related Classifications

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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.

Keywords:

Topoisomerase I/II-IN-9DNA/RNA SynthesisTopoisomerasetopoisomerase IIMGC-803colorectal carcinomagastric cancertriple negative breast cancerMDA-MB-231CT264T1 mouse triple negative breast cancer cellscGAS-STING pathwaytopoisomerase IInhibitorinhibitorinhibit

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