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Topoisomerase IIα-IN-4

Catalog No. T61431

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Topoisomerase IIα-IN-4 Chemical Structure

Topoisomerase IIα-IN-4, CAS N/A

Pack Size	Availability	Price/USD
25 mg	10-14 weeks	$ 1,520.00
50 mg	10-14 weeks	$ 1,980.00
100 mg	10-14 weeks	$ 2,500.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive inhibitor of human DNA topoisomerase II, specifically inhibiting TopoIIα with an IC50 value of 3.8 μM and TopoIIβ with an IC50 value of 10.1 μM. It demonstrates significant efficacy in inducing apoptosis and arresting the cell cycle in HepG2 cells. Moreover, Topoisomerase IIα-IN-4 exhibits robust antitumor effects against various human cancer cell lines, making it a valuable compound for cancer research [1].
In vitro	Topoisomerase IIα-IN-4 demonstrates antiproliferative effects on various cancer cell lines (including HeLa, HCT-116, MDA-MB231, HepG2, A549, CCL-226, BEAS-2B, and HL-7702) at concentrations ranging from 0-50 μM over 72 hours, with IC 50 values between 0.1 and 31.9 μM, depending on the cell line. It exhibits potent inhibitory activity specifically against Topoisomerase IIα and β, achieving IC 50 values of 3.8 and 10.1 μM, respectively. The compound acts as a non-intercalative catalytic inhibitor of Topoisomerase IIα at a concentration of 0.3 μM over 4 hours. Further, it induces cell apoptosis and cell-cycle arrest at concentrations of 0.5-1 μM over 48 and 24 hours, respectively. Interesting to note, at 0.3 μM for 4 hours in HepG2 cells, it does not affect phospho-histone H2AX levels, suggesting specific mechanisms of action without DNA damage.
In vivo	Topoisomerase IIα-IN-4 administered orally at a dosage of 500 mg/kg, twice on the first day, was observed to exhibit minimal acute toxicity in an in vivo study utilizing C57BL/6 mice (Animal Model: C57BL/6 mice [1]). The compound was administered via oral gavage at 500 mg/kg, twice on the initial day, and results indicated that it demonstrated lower toxicity in the established test without causing significant changes in the body weight of the mice.

Molecular Weight	367.44
Formula	C25H21NO2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Topoisomerase IIα-IN-4 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.