Isofistularin-3

Name: Isofistularin-3
Brand: TargetMol
SKU: T11682
Rating: 4.5 (1 reviews)

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Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin.

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	Isofistularin-3, a direct DNA-competitive DNMT1 inhibitor with an IC50 of 13.5 μM, functions as a DNA demethylating agent, leading to cell cycle arrest and increased sensitivity to TRAIL in cancer cells. Additionally, it can be employed as an ADC cytotoxin.
Targets & IC50	DNMT1:13.5 μM
In vitro	Isofistularin-3 (72 hours) inhibits a broader panel of cancer cell lines proliferation, with the GI50s ranging from 7.3-14.8 μM. Isofistularin-3 induces morphological changes and autophagy in RAJI cells. Isofistularin-3 induces caspase-dependent and -independent cell death. Isofistularin-3 sensitizes lymphoma cells to TRAIL-induced apoptosis.Isofistularin-3 (1-50 μM; 24-72 hours) shows a marked reduction of cell proliferation. Isofistularin-3 (5-50 μM; 24 hours) increases arrests cancer cells in G0/G1 cell cycle phase. Isofistularin-3 (25 μM; 72 hours) increases AHR expression. Isofistularin-3 induces AHR promoter demethylation.

Chemical Properties

Molecular Weight	1114.01
Formula	C₃₁H₃₀Br₆N₄O₁₁
Smiles	COC1=C(Br)[C@H](O)[C@@]2(ON=C(C(NC[C@H](O)COC3=C(Br)C=C([C@H](O)CNC(C4=NO[C@]5(C4)C=C(Br)C(OC)=C(Br)[C@H]5O)=O)C=C3Br)=O)C2)C=C1Br
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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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