2. Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Topoisomerase DNA/RNA Synthesis Reactive Oxygen Species (ROS) MDM-2/p53 Caspase
  4. Topoisomerase I-IN-18

Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer.

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Topoisomerase I-IN-18

Topoisomerase I-IN-18 Chemical Structure

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Topoisomerase I-IN-18 Related Antibodies

Top Publications Citing Use of Products

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Topoisomerase Topo I Topo II DNA gyrase

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RNASE L DNA Polymerases RNA Polymerases Helicases DNA Ligase

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer[1].

In Vitro

Topoisomerase I-IN-18 (Compound 11d) exhibits variable antiproliferative activity across the tested cancer cell lines, including MCF-7 (IC50 = 59.11 μM), HepG-2 (IC50 = 67.63 μM), SGC7901 (IC50 = 44.6 μM), A549 (IC50 = 8.06 μM), and exhibits minimal toxicity towards the normal HK-2 cells[1].
Topoisomerase I-IN-18 (1-10 μM) effectively blocks Topo I-mediated relaxation of superhelical DNA through dose-dependent inhibition[1].
Topoisomerase I-IN-18 (1-10 μM, 48 h) elicits dose-dependent DNA double-strand breaks in A549 cells[1].
Topoisomerase I-IN-18 (1-10 μM, 0-48 h) effectively inhibits A549 cell migration and proliferation, suggesting potential antimetastatic properties[1].
Topoisomerase I-IN-18 (4-16 μM, 48 h) induces both ROS generation and apoptosis in a dose-dependent manner in A549 cells[1].
Topoisomerase I-IN-18 (4-16 μM, 24 h) induces dose-dependent S-phase arrest accompanied by reductions in G0/G1 and G2/M populations, and significantly increases γ-H2AX phosphorylation and modulates the expression of key apoptosis-related proteins, evidenced by the upregulation of p53, Bax, caspase-3, and caspase-9 and the downregulation of Bcl-2 in A549 cells[1].
Topoisomerase I-IN-18 is identified as a P-glycoprotein (P-gp) substrate and a potential inhibitor of cytochrome P450 enzymes (CYP1A2, CYP2C19, CYP2D6, and CYP3A4)[1].

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

Topoisomerase I-IN-18 Related Antibodies

Cell Migration Assay [1]

Cell Line: A549 cells
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 0 h, 24 h, 48 h
Result: Significantly inhibited wound closure at 10 μM, while even at 2.5 μM, A549 cell migration capacity was considerably reduced.
Wound closure percentage in treated cells decreased dose-dependently with increasing concentration (from 46.25 % at 2.5 μM to 21.36 % at 10 μM).

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Dose-dependent S-phase blockade, with a decrease in the G0/G1 and G2/M phase ratios.

Western Blot Analysis[1]

Cell Line: A549 cells
Concentration: 0 μM, 4 μM, 8 μM, 16 μM
Incubation Time: 24 h
Result: Increased γ-H2AX phosphorylation levels in a dose-dependent manner, upregulated the expression of p53, Bax, caspase-3, and caspase-9, and downregulated Bcl-2 expression in A549 cells.
Molecular Weight

431.61

Formula

C23H34FN5S
SMILES

FC1=CC=C(CN2CC(CCCN3CCC4)C3C4C2CCC/C=N/NC(N)=S)C=C1
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Room temperature in continental US; may vary elsewhere.
Storage

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Purity & Documentation
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Topoisomerase I-IN-18 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-IN-18TopoisomeraseDNA/RNA SynthesisReactive Oxygen Species (ROS)MDM-2/p53CaspaseAnti-cancer agentsApoptosisCell cycleMatrine derivativesTopoisomerase I inhibitorsInhibitorinhibitorinhibit

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