| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Fat mass and obesity-associated protein (FTO).
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|---|---|
| ln Vitro |
FTO-IN-6 selectively inhibits the demethylase activity of FTO. The exact IC50 value has not been publicly disclosed, but it is designed to be a potent and selective inhibitor. By inhibiting FTO, it increases m6A levels on RNA, affecting the stability and translation of target mRNAs involved in cell proliferation and metabolism, showing potential in suppressing tumor cell proliferation.
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| Enzyme Assay |
The FTO demethylase activity assay uses recombinant FTO protein and a synthetic RNA oligonucleotide substrate containing N6-methyladenosine (m6A). The compound is pre-incubated with FTO in assay buffer. The reaction is initiated by adding the m6A-containing RNA substrate and cofactors (e.g., alpha-ketoglutarate, Fe2+, ascorbate). After incubation, the demethylation of the RNA substrate is detected and quantified by fluorescence polarization, ELISA, or LC-MS/MS measuring adenosine formation.
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| Cell Assay |
FTO-IN-6's cellular activity can be assessed using m6A-sensitive cancer cell lines (e.g., leukemia, glioblastoma). Cells are treated with varying concentrations of the compound for 48-72 hours. Cellular m6A levels are measured using an m6A ELISA-based quantification kit. Cell viability is assessed by MTT or CellTiter-Glo assays. Apoptosis is evaluated by flow cytometry with Annexin V/PI staining.
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| Animal Protocol |
In vivo activity is likely studied in murine xenograft models of cancer. Immunocompromised mice are implanted with FTO-dependent tumor cells. The compound is administered intraperitoneally or orally at multiple dose levels. Tumor growth inhibition, changes in global m6A levels in tumor tissue, and survival are monitored. Detailed published in vivo data may be available in future literature.
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data are not publicly available for FTO-IN-6. As a small molecule (MW 332.27 g/mol), its absorption, distribution, metabolism, and excretion properties would be critical to determine for in vivo studies. Its likely route of elimination is hepatic metabolism followed by renal excretion.
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| Toxicity/Toxicokinetics |
No detailed toxicology data are available for FTO-IN-6. As a research tool, cytotoxicity and off-target effects against other RNA demethylases (e.g., ALKBH5) would need to be evaluated. For potential in vivo studies, standard acute toxicity tests in rodents would be required.
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| References | |
| Additional Infomation |
FTO-IN-6 is a research chemical, not an approved drug. It is a selective FTO inhibitor used to study the role of m6A RNA modifications in cancer, obesity, and other diseases. It has shown potential in suppressing tumor cell proliferation and promoting apoptosis, particularly in leukemia and glioblastoma models, making it a valuable tool in RNA epigenetics and FTO-targeted therapeutics.
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| Molecular Formula |
C14H12N4O6
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|---|---|
| Molecular Weight |
332.26828289032
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| Exact Mass |
332.075
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| CAS # |
2968347-63-7
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| PubChem CID |
156613406
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
24
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| Complexity |
474
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC(=CC=C1NC2=NC(=C(C=C2)O)C(=O)NCC(=O)O)[N+](=O)[O-]
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| InChi Key |
ITMKUXMZMOBJES-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H12N4O6/c19-10-5-6-11(17-13(10)14(22)15-7-12(20)21)16-8-1-3-9(4-2-8)18(23)24/h1-6,19H,7H2,(H,15,22)(H,16,17)(H,20,21)
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| Chemical Name |
2-[[3-hydroxy-6-(4-nitroanilino)pyridine-2-carbonyl]amino]acetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~301.0 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.52 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0096 mL | 15.0480 mL | 30.0960 mL | |
| 5 mM | 0.6019 mL | 3.0096 mL | 6.0192 mL | |
| 10 mM | 0.3010 mL | 1.5048 mL | 3.0096 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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